CDK
Inhibitory Selectivity
Isoform-specific Inhibitors
CDK Products
| Catalog No. | Information | Product Use Citations | Product Validations |
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| S1145 |
SNS-032 (BMS-387032)SNS-032 (BMS-387032) has firstly been described as a selective inhibitor of CDK2 with IC50 of 48 nM in cell-free assays and is 10- and 20-fold selective over CDK1/CDK4. It is also found to be sensitive to CDK7/9 with IC50 of 62 nM/4 nM, with little effect on CDK6. SNS-032 (BMS-387032) induces apoptosis. Phase 1. |
HeLa cells were treated for 3h with PIK-75 or SNS-032 at the indicated concentrations. Cells were subsequently lysed and subjected to western blotting. One representative of two independent experiments is shown.
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| S1524 |
AT7519AT7519 is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM. It is less potent to CDK3 and little active to CDK7. AT7519 also inhibits GSK3β with IC50 of 89 nM. AT7519 induces apoptosis. Phase 2. |
Lysates of MDM treated with five-fold dilutions of the indicated compounds (starting concentration: AT7519, 0.5 mmol/l, roscovitine 4 mmol/l) were subjected to SDS-PAGE, transferred, and immunoblotted with antiphopho-SAMHD1, anti-SAMHD1 and anti-Hsp90 antibodies. MDM, monocyte-derived macrophage; SAMHD1, sterile a motif and HD domain-containing protein-1; SD, standard deviation.
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| S1249 |
JNJ-7706621JNJ-7706621 is pan-CDK inhibitor with the highest potency on CDK1/2 with IC50 of 9 nM/4 nM and showing >6-fold selectivity for CDK1/2 than CDK3/4/6 in cell-free assays. It also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1. |
JNJ-7706621 treatment of tamoxifen-resistant cell lines leads to arrest in the G2 cell cycle phase. M phase cells from the upper right quadrants were quantified relative to total G2/M phase cells. Statistical significant differences from vehicle-treated cells are denoted by asterisks; *P<0.05, **P<0.01.
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| S2672 |
PF-00562271 BesylatePF-00562271 Besylate (PF-562271) is the benzenesulfonate salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. Phase 1. |
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| S2621 |
AZD5438AZD5438 is a potent inhibitor of CDK1/2/9 with IC50 of 16 nM/6 nM/20 nM in cell-free assays. It is less potent to CDK5/6 and also inhibits GSK3β. Phase 1. |
(a) HEK-293 cells expressing V5-EXO1 were synchronized in different phases of the cell cycle. EXO1 was immunoprecipitated (IP) with anti-V5 antibody and Western blotted with anti-phospho-Ser (p-SP) or anti-phospho-Thr (p-TP) CDK substrate antibodies, as indicated. “+AZD” indicates cells pre-treated with the CDK inhibitor AZD5438 prior to analysis. (b) HEK-293 cells expressing V5-EXO1, synchronized in G2, were pre-treated with CDK inhibitors, AZD5438 or Roscovitine, prior to analysis of EXO1 phosphorylation by IP-Western.
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| S8816New |
PF-06873600PF-06873600 is an inhibitor of cyclin-dependent kinase 2 (CDK2), CDK4, and CDK6 with Ki values of 0.1, 1.2, and 0.1 nM, respectively, blocks the phosphorylation of retinoblastoma protein (RB1), and limits the proliferation of OVCAR-3 ovarian cancer cells with EC50s of 19 and 45 nM, respectively. |
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| E0951New |
DalpiciclibDalpiciclib (SHR-6390), a highly selective, orally bioavailable CDK4/6 inhibitor with comparable potencies against CDK4 and CDK6, exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated tumor-suppressor retinoblastoma protein (Rb) and inducing G1 cell cycle arrest. |
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| E0647New |
(R)-CR8 trihydrochloride(R)-CR8 trihydrochloride, one of CR8 isomers, is a potent inhibitor CDK1/2/5/7/9 with antiproliferative effect and proapoptotic effect on CML cell lines. |
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| S9901New |
KB-0742 DihydrochlorideKB-0742 Dihydrochloride is a potent, selective, and orally bioavailable small molecule inhibitor of the transcription elongation cofactor CDK9 with IC50 of 6 nM for CDK9/cyclin T1 inhibition at 10 μM ATP. |
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| S7371New |
Fadraciclib (CYC065)Fadraciclib (CYC065) is a novel, orally available ATP-competitive inhibitor of CDK2/CDK9 kinases with IC50 of 5 nM and 26 nM, respectively. |
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| E0072New |
Indirubin-3′-oximeIndirubin-3′-oxime (IDR3O, I3O) is an indirubin analogue that shows favorable inhibitory activity targeting GSK-3β and CDKs. Indirubin-3′-oxime also inhibits JNKs with IC50s of 0.8 μM, 1.4 μM, and 1.0 μM for JNK1, JNK2, and JNK3, respectively. Indirubin-3′-oxime activates Wnt/β-catenin signaling and inhibits adipocyte differentiation and obesity. |
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| S6884New |
LY3405105LY3405105 is an orally active CDK7 inhibitor with an IC50 of 92.8 nM. LY3405105 shows potential antineoplastic activity. |
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| S2735 |
MK-8776 (SCH 900776)MK-8776 (SCH 900776) is a selective Chk1 inhibitor with IC50 of 3 nM in a cell-free assay. It shows 500-fold selectivity against Chk2. Phase 2. |
Hela cell was trypsinized and plated at 30% confluence in DMEM. 16 hours later, MK-8776 (SCH900776) was added at final concentrations of 0, 5, 10 and 25uM. Another 24 hours later, cells were harvested in RIPA with protease and phosphatase inhibitor cocktail. Total protein concentration was measured by BCA method. Lysates equivalent to 20ug total protein were subject to Western Blot, using total- CHK1, pS345-CHK1 and beta-actin (internal control) antibodies. |
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| S2890 |
PF-562271PF-562271 (PF-00562271) is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM in cell-free assays, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. |
VEGF and P450 enzyme production in response to FAK or Src inhibitors. MCF10A cells were cultured in LD collagen gels ?vehicle control (V), 10 uM PF-562271 FAK ATP inhibitor (PF) or Src inhibitor PP2 for 24 h. Cells were also lysed and examined for CYP1A1 or CYP4B1 by immunoblot (B and C) and densitometry (D and E). VEGF data are displayed as the mean normalized to the vehicle control, N = 6, 盨EM, *p < 0.003 vs control (A). P450 data are displayed as the mean relative to GAPDH and normalized to the control. N > 4, ±SEM, *p < 0.05 vs respective control (D and E). |
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| S1487 |
PHA-793887PHA-793887 is a novel and potent inhibitor of CDK2, CDK5 and CDK7 with IC50 of 8 nM, 5 nM and 10 nM. It is greater than 6-fold more selective for CDK2, 5, and 7 than CDK1, 4, and 9. PHA-793887 induces cell-cycle arrest and apoptosis. Phase 1. |
J558 cells were treated with PHA793887 (0.02–5 umol/L) for 6 hours, after which Western blot analysis was performed to monitor XBP-1s expression. Tub, tubulin.
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| S1572 |
BS-181 HClBS-181 HCl is a highly selective CDK7 inhibitor with IC50 of 21 nM. It is more than 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9. |
Dose-response inhibition of purified human recombinant cyclin-dependent kinase CDK7/cyclin H by inhibitor BS-181 (left panel). Immunoblotting of RNA polymerase II and its phosphorylated form (at Ser5), physiological substrate of CDK7, in MCF-7 cells treated with different doses of inhibitor BS-181 for 24 h (right panel). |
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| S2670 |
A-674563A-674563 is an Akt1 inhibitor with Ki of 11 nM in cell-free assays, modest potent to PKA and >30-fold selective for Akt1 over PKC. |
B cells were pre-treated with the indicated concentrations of A-674563 for 1h prior to R848 treatment (500 ng/ml). Thymidine incorporation was analyzed 24h later. |
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| S2014 |
BMS-265246BMS-265246 is a potent and selective CDK1/2 inhibitor with IC50 of 6 nM/9 nM in a cell-free assay. It is 25-fold more selective for CDK1/2 than CDK4. |
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| S2688 |
R547R547 (Ro 4584820) is a potent ATP-competitive inhibitor of CDK1/2/4 with Ki of 2 nM/3 nM/1 nM. It is less potent to CDK7 and GSK3α/β, while inactive to other kinases. Phase 1. |
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| S7198 |
BIOBIO (GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052) is a specific inhibitor of GSK-3 with IC50 of 5 nM for GSK-3α/β in a cell-free assay, shows >16-fold selectivity over CDK5, also a pan-JAK inhibitor with IC50 of 30 nM for Tyk2. BIO induces apoptosis in human melanoma cells. |
Lysates of HCT116p53KO cells were harvested 24 hs after treatment with different GSK3 inhibitors and GSK3A/B activation/inactivation checked by western blot: a mix of pSer21-GSK3A and pSer9-GSK3B antibodies and antibody cross-reacting with both pTyr279-GSK3A and pTyr216-GSK3B were used to assess the specificity of the inhibitor for GSK3A. BIO: 6-bromoindirubin-3'-oxime, TWS: TWS119, SB2: SB216763, SB4: SB415286.
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| S6537 |
CVT-313CVT-313 is a potent CDK2 inhibitor with an IC50 of 0.5 microM in vitro. It has no effect on other, nonrelated ATP-dependent serine/threonine kinases. |
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| S0500 |
Purvalanol BPurvalanol B (NG-95) is a potent and selective inhibitor of cyclin-dependent kinase (CDK) with IC50 of 6 nM, 6 nM, 9 nM and 6 nM for cdc2-cyclin B, CDK2-cyclin A, CDK2-cyclin E and CDK5-p35, respectively. |
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| S3224 |
CinobufaginCinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis. |
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| S3238 |
ResibufogeninResibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression. |
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| S0273 |
CDK2-IN-73 (CDK2-IN-4)CDK2-IN-73 (CDK2-IN-4, CDK2 inhibitor 73) is a potent and selective inhibitor of CDK2 with IC50 of 44 nM for CDK2/cyclin A. |
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| S7549 |
THZ1 2HClTHZ1 is a covalent CDK7 inhibitor which has the unprecedented ability to target a remote cysteine residue located outside of the canonical kinase domain, providing an unanticipated means of achieving selectivity for CDK7. |
One and three days after differentiation induction, protein level of Myh3 and Myogenin were analyzed by western blot.
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| S7320 |
TG003TG003 is a potent and ATP-competitive Cdc2-like kinase (Clk) inhibitor with IC50 of 20 nM, 200 nM, and 15 nM for Clk1, Clk2, and Clk4, respectively. No inhibitory effect on Clk3, SRPK1, SRPK2, or PKC. |
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| S6540 |
NG 52NG-52 is a tri-substituted purine that binds to the ATP-binding site of yeast cyclin-dependent kinases, inhibiting Cdc28p and Pho85p with IC50s of 7 and 2 μM, respectively. |
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| S7747 |
Ro-3306RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with Ki of 20 nM, >15-fold selectivity against a diverse panel of human kinases. RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis. |
HeLa cells were untreated or treated with either colcemid (10 μg/ml for 16 h), RO-3306 (9 μM for 16 h), or both colcemid and RO-3306, as indicated. Cells were then lysed, and proteins were detected by Western analysis.
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| S7992 |
LDC4297 (LDC044297)LDC4297 is a novel CDK7 inhibitor (IC50=0.13±0.06 nM for CDK7 versus IC50s between 10 nM and 10,000 nM for all other analyzed CDKs). |
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| S8520 |
Senexin ASenexin A is a potent and selective inhibitor of CDK8 and its nearest relative, CDK19 with Kd values of 0.83 μM and 0.31 μM for CDK8 and CDK19 ATP site binding, respectively. |
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| S0771 |
BRD6989BRD6989 is a selective inhibitor of CDK8 and CDK19. BRD6989 upregulates IL-10. BRD6989 is an analog of the natural product cortistatin A (dCA). |
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| S5187 |
Ribociclib hydrochlorideRibociclib (LEE011) hydrochloride is a highly specific dual inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM, respectively. |
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| S5188 |
Ribociclib succinateRibociclib (LEE011) succinate (Kisqali) is a highly specific dual inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM, respectively. |
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| S8722 |
Samuraciclib hydrochloride (ICEC0942 hydrochloride)Samuraciclib hydrochloride (ICEC0942 hydrochloride, CT7001 hydrochloride) is a new, orally bioavailable CDK7 inhibitor with an IC50 of 40nM. The IC50 values for CDK1, CDK2, CDK5 and CDK9 were 45-, 15-, 230- and 30-fold higher. ICEC0942 (CT7001) promotes cell cycle arrest and apoptosis. |
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| S6871 |
Sodium oxamateSodium oxamate (SO, Aminooxoacetic acid, Oxamic acid) is an inhibitor of lactate dehydrogenase (LDH) that specificly inhibits LDH‑A. Sodium oxamate (SO) induces G2/M cell cycle arrest via downregulation of the CDK1/cyclin B1 pathway and promotes apoptosis through enhancement of mitochondrial ROS generation. |
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| S7969 |
THZ2THZ2, a THZ1 analog, is a selective inhibitor of CDK7 with IC50 of 13.9 nM. THZ2 efficiently suppresses the clonogenic growth of TNBC cells with IC50 of ~10 nM. |
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| S8903 |
AS2863619AS2863619 is a small-molecule cyclin-dependent kinase CDK8/19 inhibitor with IC50 of 0.6099 nM and 4.277 nM, respectively. AS2863619 is a potent Foxp3 inducer in Tconv cells. |
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| S5953 |
Menadione bisulfite sodiumMenadione(Vitamin K3) bisulfite sodium, a fat-soluble compound, is an inhibitor of Cdc25 phosphatase and mitochondrial DNA polymerase γ (pol γ), used as a nutritional supplement. |
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| S1058 |
BI-1347BI-1347 is small molecule inhibitor of Cyclin-dependent kinase 8(CDK8) with IC50 of 1.1 nM. |
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| S2009 |
Indirubin-3'-monoximeIndirubin-3'-monoxime (Indirubin-3'-oxime) is a selective CDK inhibitor with IC50 of 0.18 μM, 0.44 μM, 0.25 μM, 3.33 μM, 0.065 μM for CDK1-cyclinB, CDK2-cyclinA, CDK2-cyclinE, CDK4-cyclinD1, CDK5-p35,respectively. Indirubin-3'-monoxime is a direct and selective 5-lipoxygenase inhibitor with IC50 of 7.8-10 µM. |
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| S7793 |
Purvalanol APurvalanol A is a potent, and cell-permeable CDK inhibitor with IC50 of 4 nM, 70 nM, 35 nM, and 850 nM for cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, and cdk4-cyclin D1, respectively. Purvalanol A induces endoplasmic reticulum stress-mediated apoptosis and autophagy. |
After 12 h PAB treatment, cells were treated with PAB in the absence and presence of RO-3306 or purvalanol A for 12 h and 36 h. (A) Expressions of p-histone h3 were detected by western blot.
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| S7511 |
LY2857785LY2857785 is a type I reversible and competitive ATP kinase inhibitor against CDK9(IC50=0.011 μM) and also inhibits other transcription kinases CDK8(IC50=0.016 μM) and CDK7 (IC50=0.246 μM). |
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| S9650 |
LY3143921 hydrateLY3143921 hydrate is an orally administered ATP-competitive CDC7 inhibitor. |
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| S8894 |
SR-4835SR-4835 is a highly selective dual inhibitor of CDK12 and CDK13 with IC50 of 99 nM and Kd of 98 nM for CDK12 and IC50 of 4.9 nM for CDK13. SR-4835 disables triple-negative breast cancer (TNBC) cells. SR-4835 promotes synergy with DNA-damaging chemotherapy and PARP inhibitors. |
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| S8100 |
K03861K03861 (AUZ 454，AUZ454) is a type II CDK2 inhibitor with Kd of 50 nM, 18.6 nM, 15.4 nM, and 9.7 nM for CDK2(WT), CDK2(C118L), CDK2(A144C), and CDK2(C118L/A144C), respectlvely. |
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| S9742 |
IndisulamIndisulam (E7070), a sulfonamide anticancer agent, is a potent carbonic anhydrase (CA) inhibitor that inhibits cytosolic isozymes I and II, and transmembrane, tumor-associated isozyme IX. Indisulam suppresses the expression of cyclin E and phosphorylation of CDK2, both of which are essential for the G1 to S transition. |
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| S0354 |
AlsterpaulloneAlsterpaullone (Alp, 9-Nitropaullone, NSC 705701) is a potent inhibitor of CDK with IC50 of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also acts as a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 of both 4 nM for GSK-3α and GSK-3β. Alsterpaullone induces apoptosis by activation of caspase-9. Alsterpaullone has antitumor activity and possesses potential for the treatment of neurodegenerative and proliferative disorders. |
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| S8389 |
Trilaciclib (G1T28)Trilaciclib (G1T28, G1T28-1) is a highly potent, selective and reversible cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitor. Trilaciclib inhibits CDK4/cyclin D1 and CDK6/cyclin D3 with IC50 of 1 nM and 4 nM, respectively. |
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| S7773 |
CDKI-73CDKI-73 (LS-007) is a potent CDK inhibitor in vitro with IC50 of 8.17 nM, 3.27 nM, 8.18 nM, and 5.78 nM for CDK1, CDK2, CDK4, and CDK9, respectively. CDKI-73 induces apoptosis in cancer cells. CDKI-73 is an orally bioavailable and highly efficacious CDK9 inhibitor against acute myeloid leukemia. |
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| S7648 |
OTS964OTS964 is a potent TOPK inhibitor with high affinity and selectivity and IC50 value is 28 nM. OTS964 is also a potent inhibitor of the cyclin-dependent kinase CDK11 with Kd of 40 nM. OTS964 treatment activates autophagy in glioma cells and induces apoptosis of human lung cancer cells in mouse xenografts. |
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| S8783 |
JSH-150JSH-150 is a highly selective and potent inhibitor of CDK9 with IC50 of 1 nM. |
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| S8809 |
MC180295MC180295 ((rel)-MC180295) is a novel potent and selective CDK9 inhibitor with an IC50 of 5 nM and is at least 22-fold more selective for CDK9 over other CDKs. |
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| S7509 |
ML167ML167 (CID 44968231) is a highly selective Cdc2-like kinase 4 (Clk4) inhibitor with IC50 of 136 nM, >10-fold selectivity for closely related kinases Clk1-3 and Dyrk1A/1B. |
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| S6885 |
AilanthoneAilanthone (AIL, Δ13-Dehydrochaparrinone), a natural anti-hepatocellular carcinoma (HCC) component in Ailanthus altissima, induces G0/G1-phase cell cycle arrest by decreasing expression of cyclins and CDKs and increases expression of p21 and p27. Ailanthone triggers DNA damage characterized by activation of the ATM/ATR pathway. Ailanthone induces apoptosis which is mitochondrion-mediated and involves the PI3K/AKT signaling pathway in Huh7 cells. Ailanthone is also a potent inhibitor of both full-length Androgen Receptor (AR-FL) and constitutively active truncated AR splice variants (AR-Vs, AR1-651) with IC50 of 69 nM and 309 nM, respectively. |
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| S7461 |
LDC000067LDC000067 (LDC067) is a highly selective CDK9 inhibitor with IC50 of 44 nM, 55/125/210/ >227/ >227-fold selectivity over CDK2/1/4/6/7. |
Inhibition of CDK9 leads to a decrease in RNApol II activity and repetitive element expression. HEK293T cells were treated with DMSO control and the indicated amounts of LDC000067, a CDK9 inhibitor, for a total of 3 h. (A) Immunoblots showing the levels of phosphorylated RNApol II largest subunit (pRPB1), total RPB1 and GAPDH, in response to different doses of CDK9 inhibitor. (B) Quantification of immunoblots from 2 independent experiments in which each condition was performed in duplicates, and in which pRPB1 and total RPB1 protein levels were normalized to GAPDH or as pRPB1/Total RPB1 ratio. (C, D) qRT-PCR analyses show a significant response to CDK9 inhibition of repetitive elements belonging to the LTR (C) and SINE (D) classes. Statistical analyses were performed to compare all groups using a One-way ANOVA followed by Bonforreoni’s multiple comparison test, *P < 0.05, **P < 0.01, #P < 0.0001. |
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| S9665 |
Motixafortide (BL-8040)Motixafortide (BL-8040, BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140) is an antagonist of CXCR4 with IC50 of ～1 nM. BL-8040 induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a/16-1 expression. |
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| S8979 |
THAL-SNS-032THAL-SNS-032 is a selective Cyclin-dependent kinase 9 (CDK9) degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN). |
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| S8981 |
NVP-2NVP-2, a potent, selective, non-neurotoxic and ATP-competitive cyclin dependent kinase 9 (CDK9) inhibitor with IC50 of 0.514 nM for CDK9/CycT activity and induces cell apoptosis. |
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| S4454 |
FIT-039FIT-039 is a potent inhibitor of cyclin-dependent kinase 9 (CDK9), suppressing replication of a broad spectrum of DNA viruses through inhibition of mRNA transcription. |
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| S8730 |
BAY 1251152BAY1251152 is a potent PTEFb/CDK9 inhibitor with an IC50 value of 3 nM for CDK9 and an at least 50-fold selectivity against other CDKs in enzymatic assays. BAY1251152 binds to and blocks the phosphorylation and kinase activity of CDK9, thereby preventing PTEFb-mediated activation of RNA Pol II and leading to the inhibition of gene transcription of various anti-apoptotic proteins. |
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| S9605 |
ApcinApcin (APC inhibitor) is an inhibitor of the E3 ligase activity of the mitotic anaphase-promoting complex/cyclosome (APC/C) that binds to Cdc20 and competitively inhibits the ubiquitylation of D-box-containing substrates. |
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| S8863 |
YKL-5-124YKL-5-124 is a potent, selective and covalent CDK7 inhibitor with an IC50 of 9.7 nM, 1300 nM and 3020 nM for inhibiting CDK7/Mat1/CycH, CDK2 and CDK9 respectively. It displays biochemical and cellular selectivity for CDK7 over CDK12/13. |
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| S8719 |
AZD4573AZD4573 is a potent inhibitor of CDK9 (IC50 of <0.004 μM) with fast-off binding kinetics (t1/2 = 16 min) and high selectivity versus other kinases, including other CDK family kinases. |
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| S7547 |
XL413 (BMS-863233)XL413 (BMS-863233) is a potent and selective cell division cycle 7 homolog (CDC7) kinase inhibitor with IC50 of 3.4 nM, showing 63-, 12- and 35-fold selectivity over CK2, Pim-1 and pMCM2, respectively. Phase 1/2. |
The protein levels of p-MCM2 and p-ERK in NOK, HN6 and Cal27 cells treated with 0, 10 and 20 μMXL413 were detected by western blotting.
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| S2642 |
1-Naphthyl PP1(1-NA-PP1)1-Naphthyl PP1(1-NA-PP 1) is a highly selective and potent pan-PKD inhibitor with IC50 of 154.6 nM,133.4 nM and 109.4 nM for PKD1, PKD2 and PKD3, respectively. 1-Naphthyl PP1 is a selective inhibitor of Src family kinases (v-Src, c-Fyn) and the tyrosine kinase c-Abl with IC50 of 1.0 μM, 0.6 μM, 0.6 μM, 18 μM and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II, respectively. |
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| S8840 |
SEL120 (SEL120-34A) hydrochlorideSEL120 (SEL120-34, SEL120-34A) is a novel inhibitor of Cyclin-dependent kinase 8 (CDK8) with IC50 values of 4.4 nM and 10.4 nM for CDK8/Cyclin C and CDK19/CyclinC respectively. |
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| S6595 |
THZ531THZ531 is a selective covalent inhibitor of CDK12 and CDK13 with IC50 values of 158 and 69 nM, respectively. |
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| S8815 |
BSJ-03-123BSJ-03-123 is a phthalimide-based degrader of cyclin-dependent kinase 6 (CDK6). (PROTAC) |
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| S6383 |
1-NM-PP11-NM-PP1 (PP1 Analog II, 1NM-PP1, analogue 9) is a potent inhibitor of Src family kinases with IC50 of 4.3 nM and 3.2 nM for v-Src-as1 and c-Fyn-as1, respectively. 1-NM-PP1 also inhibits CDK2-as1, CAMKII-as1 and c-Abl-as2 with IC50 of 5.0 nM, 8.0 nM and 120 nM, respectively. |
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| S6768 |
CC-671CC-671 is a selectively dual inhibitor of TTK (human protein kinase monopolar spindle 1 [hMps1]) and CDC like kinase 2 (CLK2) with IC50s of 5 nM and 3 nM for TTK and CLK2, respectively. |
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| S4482 |
PalbociclibPalbociclib (Ibrance, PD 0332991) is a highly specific inhibitor of cyclin-dependent kinase 4 (Cdk4) and Cdk6 with IC50 of 11 nM and 16 nM, respectively. |
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| S6777 |
NSC95397NSC 95397 is a potent, selective Cdc25 dual specificity phosphatase inhibitor with Ki of 32 nM, 96 nM, 40 nM for Cdc25A, Cdc25B and Cdc25C, respectively. NSC 95397 has IC50 of 22.3 nM, 56.9 nM and 125 nM for human Cdc25A, human Cdc25C and Cdc25B, respectively. NSC 95397 inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) and suppresses proliferation and induces apoptosis in colon cancer cells through MKP-1 and ERK1/2 pathway. |
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| S9859 |
BSJ-4-116BSJ-4-116 is a specific degrader of cyclin-dependent kinase 12 (CDK12). BSJ-4-116 exhibits potent antiproliferative effects. |
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| S9880 |
MS140MS140 is a specific and highly potent CDK4/6 kinase inhibitor and also a CDK4/6 degrader (PROTAC). |
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| S7981 |
CCT251545CCT251545 is a potent, orally bioavailable inhibitor of WNT signaling with IC50 of 5 nM in 7dF3 cells. CCT251545 also act as a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease. |
| Catalog No. | Information | Product Use Citations | Product Validations |
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| S1145 |
SNS-032 (BMS-387032)SNS-032 (BMS-387032) has firstly been described as a selective inhibitor of CDK2 with IC50 of 48 nM in cell-free assays and is 10- and 20-fold selective over CDK1/CDK4. It is also found to be sensitive to CDK7/9 with IC50 of 62 nM/4 nM, with little effect on CDK6. SNS-032 (BMS-387032) induces apoptosis. Phase 1. |
HeLa cells were treated for 3h with PIK-75 or SNS-032 at the indicated concentrations. Cells were subsequently lysed and subjected to western blotting. One representative of two independent experiments is shown.
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| S1524 |
AT7519AT7519 is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM. It is less potent to CDK3 and little active to CDK7. AT7519 also inhibits GSK3β with IC50 of 89 nM. AT7519 induces apoptosis. Phase 2. |
Lysates of MDM treated with five-fold dilutions of the indicated compounds (starting concentration: AT7519, 0.5 mmol/l, roscovitine 4 mmol/l) were subjected to SDS-PAGE, transferred, and immunoblotted with antiphopho-SAMHD1, anti-SAMHD1 and anti-Hsp90 antibodies. MDM, monocyte-derived macrophage; SAMHD1, sterile a motif and HD domain-containing protein-1; SD, standard deviation.
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| S1249 |
JNJ-7706621JNJ-7706621 is pan-CDK inhibitor with the highest potency on CDK1/2 with IC50 of 9 nM/4 nM and showing >6-fold selectivity for CDK1/2 than CDK3/4/6 in cell-free assays. It also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1. |
JNJ-7706621 treatment of tamoxifen-resistant cell lines leads to arrest in the G2 cell cycle phase. M phase cells from the upper right quadrants were quantified relative to total G2/M phase cells. Statistical significant differences from vehicle-treated cells are denoted by asterisks; *P<0.05, **P<0.01.
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| S2672 |
PF-00562271 BesylatePF-00562271 Besylate (PF-562271) is the benzenesulfonate salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. Phase 1. |
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| S2621 |
AZD5438AZD5438 is a potent inhibitor of CDK1/2/9 with IC50 of 16 nM/6 nM/20 nM in cell-free assays. It is less potent to CDK5/6 and also inhibits GSK3β. Phase 1. |
(a) HEK-293 cells expressing V5-EXO1 were synchronized in different phases of the cell cycle. EXO1 was immunoprecipitated (IP) with anti-V5 antibody and Western blotted with anti-phospho-Ser (p-SP) or anti-phospho-Thr (p-TP) CDK substrate antibodies, as indicated. “+AZD” indicates cells pre-treated with the CDK inhibitor AZD5438 prior to analysis. (b) HEK-293 cells expressing V5-EXO1, synchronized in G2, were pre-treated with CDK inhibitors, AZD5438 or Roscovitine, prior to analysis of EXO1 phosphorylation by IP-Western.
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| S8816New |
PF-06873600PF-06873600 is an inhibitor of cyclin-dependent kinase 2 (CDK2), CDK4, and CDK6 with Ki values of 0.1, 1.2, and 0.1 nM, respectively, blocks the phosphorylation of retinoblastoma protein (RB1), and limits the proliferation of OVCAR-3 ovarian cancer cells with EC50s of 19 and 45 nM, respectively. |
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| E0951New |
DalpiciclibDalpiciclib (SHR-6390), a highly selective, orally bioavailable CDK4/6 inhibitor with comparable potencies against CDK4 and CDK6, exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated tumor-suppressor retinoblastoma protein (Rb) and inducing G1 cell cycle arrest. |
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| E0647New |
(R)-CR8 trihydrochloride(R)-CR8 trihydrochloride, one of CR8 isomers, is a potent inhibitor CDK1/2/5/7/9 with antiproliferative effect and proapoptotic effect on CML cell lines. |
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| S9901New |
KB-0742 DihydrochlorideKB-0742 Dihydrochloride is a potent, selective, and orally bioavailable small molecule inhibitor of the transcription elongation cofactor CDK9 with IC50 of 6 nM for CDK9/cyclin T1 inhibition at 10 μM ATP. |
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| S7371New |
Fadraciclib (CYC065)Fadraciclib (CYC065) is a novel, orally available ATP-competitive inhibitor of CDK2/CDK9 kinases with IC50 of 5 nM and 26 nM, respectively. |
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| E0072New |
Indirubin-3′-oximeIndirubin-3′-oxime (IDR3O, I3O) is an indirubin analogue that shows favorable inhibitory activity targeting GSK-3β and CDKs. Indirubin-3′-oxime also inhibits JNKs with IC50s of 0.8 μM, 1.4 μM, and 1.0 μM for JNK1, JNK2, and JNK3, respectively. Indirubin-3′-oxime activates Wnt/β-catenin signaling and inhibits adipocyte differentiation and obesity. |
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| S6884New |
LY3405105LY3405105 is an orally active CDK7 inhibitor with an IC50 of 92.8 nM. LY3405105 shows potential antineoplastic activity. |
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| S2735 |
MK-8776 (SCH 900776)MK-8776 (SCH 900776) is a selective Chk1 inhibitor with IC50 of 3 nM in a cell-free assay. It shows 500-fold selectivity against Chk2. Phase 2. |
Hela cell was trypsinized and plated at 30% confluence in DMEM. 16 hours later, MK-8776 (SCH900776) was added at final concentrations of 0, 5, 10 and 25uM. Another 24 hours later, cells were harvested in RIPA with protease and phosphatase inhibitor cocktail. Total protein concentration was measured by BCA method. Lysates equivalent to 20ug total protein were subject to Western Blot, using total- CHK1, pS345-CHK1 and beta-actin (internal control) antibodies. |
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| S2890 |
PF-562271PF-562271 (PF-00562271) is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM in cell-free assays, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. |
VEGF and P450 enzyme production in response to FAK or Src inhibitors. MCF10A cells were cultured in LD collagen gels ?vehicle control (V), 10 uM PF-562271 FAK ATP inhibitor (PF) or Src inhibitor PP2 for 24 h. Cells were also lysed and examined for CYP1A1 or CYP4B1 by immunoblot (B and C) and densitometry (D and E). VEGF data are displayed as the mean normalized to the vehicle control, N = 6, 盨EM, *p < 0.003 vs control (A). P450 data are displayed as the mean relative to GAPDH and normalized to the control. N > 4, ±SEM, *p < 0.05 vs respective control (D and E). |
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| S1487 |
PHA-793887PHA-793887 is a novel and potent inhibitor of CDK2, CDK5 and CDK7 with IC50 of 8 nM, 5 nM and 10 nM. It is greater than 6-fold more selective for CDK2, 5, and 7 than CDK1, 4, and 9. PHA-793887 induces cell-cycle arrest and apoptosis. Phase 1. |
J558 cells were treated with PHA793887 (0.02–5 umol/L) for 6 hours, after which Western blot analysis was performed to monitor XBP-1s expression. Tub, tubulin.
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| S1572 |
BS-181 HClBS-181 HCl is a highly selective CDK7 inhibitor with IC50 of 21 nM. It is more than 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9. |
Dose-response inhibition of purified human recombinant cyclin-dependent kinase CDK7/cyclin H by inhibitor BS-181 (left panel). Immunoblotting of RNA polymerase II and its phosphorylated form (at Ser5), physiological substrate of CDK7, in MCF-7 cells treated with different doses of inhibitor BS-181 for 24 h (right panel). |
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| S2670 |
A-674563A-674563 is an Akt1 inhibitor with Ki of 11 nM in cell-free assays, modest potent to PKA and >30-fold selective for Akt1 over PKC. |
B cells were pre-treated with the indicated concentrations of A-674563 for 1h prior to R848 treatment (500 ng/ml). Thymidine incorporation was analyzed 24h later. |
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| S2014 |
BMS-265246BMS-265246 is a potent and selective CDK1/2 inhibitor with IC50 of 6 nM/9 nM in a cell-free assay. It is 25-fold more selective for CDK1/2 than CDK4. |
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| S2688 |
R547R547 (Ro 4584820) is a potent ATP-competitive inhibitor of CDK1/2/4 with Ki of 2 nM/3 nM/1 nM. It is less potent to CDK7 and GSK3α/β, while inactive to other kinases. Phase 1. |
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| S7198 |
BIOBIO (GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052) is a specific inhibitor of GSK-3 with IC50 of 5 nM for GSK-3α/β in a cell-free assay, shows >16-fold selectivity over CDK5, also a pan-JAK inhibitor with IC50 of 30 nM for Tyk2. BIO induces apoptosis in human melanoma cells. |
Lysates of HCT116p53KO cells were harvested 24 hs after treatment with different GSK3 inhibitors and GSK3A/B activation/inactivation checked by western blot: a mix of pSer21-GSK3A and pSer9-GSK3B antibodies and antibody cross-reacting with both pTyr279-GSK3A and pTyr216-GSK3B were used to assess the specificity of the inhibitor for GSK3A. BIO: 6-bromoindirubin-3'-oxime, TWS: TWS119, SB2: SB216763, SB4: SB415286.
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| S6537 |
CVT-313CVT-313 is a potent CDK2 inhibitor with an IC50 of 0.5 microM in vitro. It has no effect on other, nonrelated ATP-dependent serine/threonine kinases. |
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| S0500 |
Purvalanol BPurvalanol B (NG-95) is a potent and selective inhibitor of cyclin-dependent kinase (CDK) with IC50 of 6 nM, 6 nM, 9 nM and 6 nM for cdc2-cyclin B, CDK2-cyclin A, CDK2-cyclin E and CDK5-p35, respectively. |
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| S3224 |
CinobufaginCinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis. |
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| S3238 |
ResibufogeninResibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression. |
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| S0273 |
CDK2-IN-73 (CDK2-IN-4)CDK2-IN-73 (CDK2-IN-4, CDK2 inhibitor 73) is a potent and selective inhibitor of CDK2 with IC50 of 44 nM for CDK2/cyclin A. |
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| S7549 |
THZ1 2HClTHZ1 is a covalent CDK7 inhibitor which has the unprecedented ability to target a remote cysteine residue located outside of the canonical kinase domain, providing an unanticipated means of achieving selectivity for CDK7. |
One and three days after differentiation induction, protein level of Myh3 and Myogenin were analyzed by western blot.
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| S7320 |
TG003TG003 is a potent and ATP-competitive Cdc2-like kinase (Clk) inhibitor with IC50 of 20 nM, 200 nM, and 15 nM for Clk1, Clk2, and Clk4, respectively. No inhibitory effect on Clk3, SRPK1, SRPK2, or PKC. |
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| S6540 |
NG 52NG-52 is a tri-substituted purine that binds to the ATP-binding site of yeast cyclin-dependent kinases, inhibiting Cdc28p and Pho85p with IC50s of 7 and 2 μM, respectively. |
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| S7747 |
Ro-3306RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with Ki of 20 nM, >15-fold selectivity against a diverse panel of human kinases. RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis. |
HeLa cells were untreated or treated with either colcemid (10 μg/ml for 16 h), RO-3306 (9 μM for 16 h), or both colcemid and RO-3306, as indicated. Cells were then lysed, and proteins were detected by Western analysis.
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| S7992 |
LDC4297 (LDC044297)LDC4297 is a novel CDK7 inhibitor (IC50=0.13±0.06 nM for CDK7 versus IC50s between 10 nM and 10,000 nM for all other analyzed CDKs). |
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| S8520 |
Senexin ASenexin A is a potent and selective inhibitor of CDK8 and its nearest relative, CDK19 with Kd values of 0.83 μM and 0.31 μM for CDK8 and CDK19 ATP site binding, respectively. |
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| S0771 |
BRD6989BRD6989 is a selective inhibitor of CDK8 and CDK19. BRD6989 upregulates IL-10. BRD6989 is an analog of the natural product cortistatin A (dCA). |
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| S5187 |
Ribociclib hydrochlorideRibociclib (LEE011) hydrochloride is a highly specific dual inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM, respectively. |
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| S5188 |
Ribociclib succinateRibociclib (LEE011) succinate (Kisqali) is a highly specific dual inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM, respectively. |
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| S8722 |
Samuraciclib hydrochloride (ICEC0942 hydrochloride)Samuraciclib hydrochloride (ICEC0942 hydrochloride, CT7001 hydrochloride) is a new, orally bioavailable CDK7 inhibitor with an IC50 of 40nM. The IC50 values for CDK1, CDK2, CDK5 and CDK9 were 45-, 15-, 230- and 30-fold higher. ICEC0942 (CT7001) promotes cell cycle arrest and apoptosis. |
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| S6871 |
Sodium oxamateSodium oxamate (SO, Aminooxoacetic acid, Oxamic acid) is an inhibitor of lactate dehydrogenase (LDH) that specificly inhibits LDH‑A. Sodium oxamate (SO) induces G2/M cell cycle arrest via downregulation of the CDK1/cyclin B1 pathway and promotes apoptosis through enhancement of mitochondrial ROS generation. |
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| S7969 |
THZ2THZ2, a THZ1 analog, is a selective inhibitor of CDK7 with IC50 of 13.9 nM. THZ2 efficiently suppresses the clonogenic growth of TNBC cells with IC50 of ~10 nM. |
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| S8903 |
AS2863619AS2863619 is a small-molecule cyclin-dependent kinase CDK8/19 inhibitor with IC50 of 0.6099 nM and 4.277 nM, respectively. AS2863619 is a potent Foxp3 inducer in Tconv cells. |
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| S5953 |
Menadione bisulfite sodiumMenadione(Vitamin K3) bisulfite sodium, a fat-soluble compound, is an inhibitor of Cdc25 phosphatase and mitochondrial DNA polymerase γ (pol γ), used as a nutritional supplement. |
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| S1058 |
BI-1347BI-1347 is small molecule inhibitor of Cyclin-dependent kinase 8(CDK8) with IC50 of 1.1 nM. |
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| S2009 |
Indirubin-3'-monoximeIndirubin-3'-monoxime (Indirubin-3'-oxime) is a selective CDK inhibitor with IC50 of 0.18 μM, 0.44 μM, 0.25 μM, 3.33 μM, 0.065 μM for CDK1-cyclinB, CDK2-cyclinA, CDK2-cyclinE, CDK4-cyclinD1, CDK5-p35,respectively. Indirubin-3'-monoxime is a direct and selective 5-lipoxygenase inhibitor with IC50 of 7.8-10 µM. |
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| S7793 |
Purvalanol APurvalanol A is a potent, and cell-permeable CDK inhibitor with IC50 of 4 nM, 70 nM, 35 nM, and 850 nM for cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, and cdk4-cyclin D1, respectively. Purvalanol A induces endoplasmic reticulum stress-mediated apoptosis and autophagy. |
After 12 h PAB treatment, cells were treated with PAB in the absence and presence of RO-3306 or purvalanol A for 12 h and 36 h. (A) Expressions of p-histone h3 were detected by western blot.
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| S7511 |
LY2857785LY2857785 is a type I reversible and competitive ATP kinase inhibitor against CDK9(IC50=0.011 μM) and also inhibits other transcription kinases CDK8(IC50=0.016 μM) and CDK7 (IC50=0.246 μM). |
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| S9650 |
LY3143921 hydrateLY3143921 hydrate is an orally administered ATP-competitive CDC7 inhibitor. |
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| S8894 |
SR-4835SR-4835 is a highly selective dual inhibitor of CDK12 and CDK13 with IC50 of 99 nM and Kd of 98 nM for CDK12 and IC50 of 4.9 nM for CDK13. SR-4835 disables triple-negative breast cancer (TNBC) cells. SR-4835 promotes synergy with DNA-damaging chemotherapy and PARP inhibitors. |
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| S8100 |
K03861K03861 (AUZ 454，AUZ454) is a type II CDK2 inhibitor with Kd of 50 nM, 18.6 nM, 15.4 nM, and 9.7 nM for CDK2(WT), CDK2(C118L), CDK2(A144C), and CDK2(C118L/A144C), respectlvely. |
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| S9742 |
IndisulamIndisulam (E7070), a sulfonamide anticancer agent, is a potent carbonic anhydrase (CA) inhibitor that inhibits cytosolic isozymes I and II, and transmembrane, tumor-associated isozyme IX. Indisulam suppresses the expression of cyclin E and phosphorylation of CDK2, both of which are essential for the G1 to S transition. |
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| S0354 |
AlsterpaulloneAlsterpaullone (Alp, 9-Nitropaullone, NSC 705701) is a potent inhibitor of CDK with IC50 of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also acts as a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 of both 4 nM for GSK-3α and GSK-3β. Alsterpaullone induces apoptosis by activation of caspase-9. Alsterpaullone has antitumor activity and possesses potential for the treatment of neurodegenerative and proliferative disorders. |
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| S8389 |
Trilaciclib (G1T28)Trilaciclib (G1T28, G1T28-1) is a highly potent, selective and reversible cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitor. Trilaciclib inhibits CDK4/cyclin D1 and CDK6/cyclin D3 with IC50 of 1 nM and 4 nM, respectively. |
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| S7773 |
CDKI-73CDKI-73 (LS-007) is a potent CDK inhibitor in vitro with IC50 of 8.17 nM, 3.27 nM, 8.18 nM, and 5.78 nM for CDK1, CDK2, CDK4, and CDK9, respectively. CDKI-73 induces apoptosis in cancer cells. CDKI-73 is an orally bioavailable and highly efficacious CDK9 inhibitor against acute myeloid leukemia. |
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| S7648 |
OTS964OTS964 is a potent TOPK inhibitor with high affinity and selectivity and IC50 value is 28 nM. OTS964 is also a potent inhibitor of the cyclin-dependent kinase CDK11 with Kd of 40 nM. OTS964 treatment activates autophagy in glioma cells and induces apoptosis of human lung cancer cells in mouse xenografts. |
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| S8783 |
JSH-150JSH-150 is a highly selective and potent inhibitor of CDK9 with IC50 of 1 nM. |
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| S8809 |
MC180295MC180295 ((rel)-MC180295) is a novel potent and selective CDK9 inhibitor with an IC50 of 5 nM and is at least 22-fold more selective for CDK9 over other CDKs. |
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| S7509 |
ML167ML167 (CID 44968231) is a highly selective Cdc2-like kinase 4 (Clk4) inhibitor with IC50 of 136 nM, >10-fold selectivity for closely related kinases Clk1-3 and Dyrk1A/1B. |
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| S6885 |
AilanthoneAilanthone (AIL, Δ13-Dehydrochaparrinone), a natural anti-hepatocellular carcinoma (HCC) component in Ailanthus altissima, induces G0/G1-phase cell cycle arrest by decreasing expression of cyclins and CDKs and increases expression of p21 and p27. Ailanthone triggers DNA damage characterized by activation of the ATM/ATR pathway. Ailanthone induces apoptosis which is mitochondrion-mediated and involves the PI3K/AKT signaling pathway in Huh7 cells. Ailanthone is also a potent inhibitor of both full-length Androgen Receptor (AR-FL) and constitutively active truncated AR splice variants (AR-Vs, AR1-651) with IC50 of 69 nM and 309 nM, respectively. |
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| S7461 |
LDC000067LDC000067 (LDC067) is a highly selective CDK9 inhibitor with IC50 of 44 nM, 55/125/210/ >227/ >227-fold selectivity over CDK2/1/4/6/7. |
Inhibition of CDK9 leads to a decrease in RNApol II activity and repetitive element expression. HEK293T cells were treated with DMSO control and the indicated amounts of LDC000067, a CDK9 inhibitor, for a total of 3 h. (A) Immunoblots showing the levels of phosphorylated RNApol II largest subunit (pRPB1), total RPB1 and GAPDH, in response to different doses of CDK9 inhibitor. (B) Quantification of immunoblots from 2 independent experiments in which each condition was performed in duplicates, and in which pRPB1 and total RPB1 protein levels were normalized to GAPDH or as pRPB1/Total RPB1 ratio. (C, D) qRT-PCR analyses show a significant response to CDK9 inhibition of repetitive elements belonging to the LTR (C) and SINE (D) classes. Statistical analyses were performed to compare all groups using a One-way ANOVA followed by Bonforreoni’s multiple comparison test, *P < 0.05, **P < 0.01, #P < 0.0001. |
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| S9665 |
Motixafortide (BL-8040)Motixafortide (BL-8040, BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140) is an antagonist of CXCR4 with IC50 of ～1 nM. BL-8040 induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a/16-1 expression. |
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| S8979 |
THAL-SNS-032THAL-SNS-032 is a selective Cyclin-dependent kinase 9 (CDK9) degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN). |
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| S8981 |
NVP-2NVP-2, a potent, selective, non-neurotoxic and ATP-competitive cyclin dependent kinase 9 (CDK9) inhibitor with IC50 of 0.514 nM for CDK9/CycT activity and induces cell apoptosis. |
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| S4454 |
FIT-039FIT-039 is a potent inhibitor of cyclin-dependent kinase 9 (CDK9), suppressing replication of a broad spectrum of DNA viruses through inhibition of mRNA transcription. |
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| S8730 |
BAY 1251152BAY1251152 is a potent PTEFb/CDK9 inhibitor with an IC50 value of 3 nM for CDK9 and an at least 50-fold selectivity against other CDKs in enzymatic assays. BAY1251152 binds to and blocks the phosphorylation and kinase activity of CDK9, thereby preventing PTEFb-mediated activation of RNA Pol II and leading to the inhibition of gene transcription of various anti-apoptotic proteins. |
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| S9605 |
ApcinApcin (APC inhibitor) is an inhibitor of the E3 ligase activity of the mitotic anaphase-promoting complex/cyclosome (APC/C) that binds to Cdc20 and competitively inhibits the ubiquitylation of D-box-containing substrates. |
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| S8863 |
YKL-5-124YKL-5-124 is a potent, selective and covalent CDK7 inhibitor with an IC50 of 9.7 nM, 1300 nM and 3020 nM for inhibiting CDK7/Mat1/CycH, CDK2 and CDK9 respectively. It displays biochemical and cellular selectivity for CDK7 over CDK12/13. |
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| S8719 |
AZD4573AZD4573 is a potent inhibitor of CDK9 (IC50 of <0.004 μM) with fast-off binding kinetics (t1/2 = 16 min) and high selectivity versus other kinases, including other CDK family kinases. |
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| S7547 |
XL413 (BMS-863233)XL413 (BMS-863233) is a potent and selective cell division cycle 7 homolog (CDC7) kinase inhibitor with IC50 of 3.4 nM, showing 63-, 12- and 35-fold selectivity over CK2, Pim-1 and pMCM2, respectively. Phase 1/2. |
The protein levels of p-MCM2 and p-ERK in NOK, HN6 and Cal27 cells treated with 0, 10 and 20 μMXL413 were detected by western blotting.
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| S2642 |
1-Naphthyl PP1(1-NA-PP1)1-Naphthyl PP1(1-NA-PP 1) is a highly selective and potent pan-PKD inhibitor with IC50 of 154.6 nM,133.4 nM and 109.4 nM for PKD1, PKD2 and PKD3, respectively. 1-Naphthyl PP1 is a selective inhibitor of Src family kinases (v-Src, c-Fyn) and the tyrosine kinase c-Abl with IC50 of 1.0 μM, 0.6 μM, 0.6 μM, 18 μM and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II, respectively. |
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| S8840 |
SEL120 (SEL120-34A) hydrochlorideSEL120 (SEL120-34, SEL120-34A) is a novel inhibitor of Cyclin-dependent kinase 8 (CDK8) with IC50 values of 4.4 nM and 10.4 nM for CDK8/Cyclin C and CDK19/CyclinC respectively. |
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| S6595 |
THZ531THZ531 is a selective covalent inhibitor of CDK12 and CDK13 with IC50 values of 158 and 69 nM, respectively. |
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| S8815 |
BSJ-03-123BSJ-03-123 is a phthalimide-based degrader of cyclin-dependent kinase 6 (CDK6). (PROTAC) |
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| S6383 |
1-NM-PP11-NM-PP1 (PP1 Analog II, 1NM-PP1, analogue 9) is a potent inhibitor of Src family kinases with IC50 of 4.3 nM and 3.2 nM for v-Src-as1 and c-Fyn-as1, respectively. 1-NM-PP1 also inhibits CDK2-as1, CAMKII-as1 and c-Abl-as2 with IC50 of 5.0 nM, 8.0 nM and 120 nM, respectively. |
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| S6768 |
CC-671CC-671 is a selectively dual inhibitor of TTK (human protein kinase monopolar spindle 1 [hMps1]) and CDC like kinase 2 (CLK2) with IC50s of 5 nM and 3 nM for TTK and CLK2, respectively. |
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| S4482 |
PalbociclibPalbociclib (Ibrance, PD 0332991) is a highly specific inhibitor of cyclin-dependent kinase 4 (Cdk4) and Cdk6 with IC50 of 11 nM and 16 nM, respectively. |
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| S6777 |
NSC95397NSC 95397 is a potent, selective Cdc25 dual specificity phosphatase inhibitor with Ki of 32 nM, 96 nM, 40 nM for Cdc25A, Cdc25B and Cdc25C, respectively. NSC 95397 has IC50 of 22.3 nM, 56.9 nM and 125 nM for human Cdc25A, human Cdc25C and Cdc25B, respectively. NSC 95397 inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) and suppresses proliferation and induces apoptosis in colon cancer cells through MKP-1 and ERK1/2 pathway. |
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| S9859 |
BSJ-4-116BSJ-4-116 is a specific degrader of cyclin-dependent kinase 12 (CDK12). BSJ-4-116 exhibits potent antiproliferative effects. |
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| S9880 |
MS140MS140 is a specific and highly potent CDK4/6 kinase inhibitor and also a CDK4/6 degrader (PROTAC). |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S7981 |
CCT251545CCT251545 is a potent, orally bioavailable inhibitor of WNT signaling with IC50 of 5 nM in 7dF3 cells. CCT251545 also act as a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease. |
