New Products

PI3K/Akt/mTOR
Catalog No. Product Name Information Added
E0121 Parsaclisib (INCB050465)

Parsaclisib (INCB050465, INCB-50465, IBI376) is a potent and highly selective PI3Kδ(PI3K delta) inhibitor with an IC50 of 1 nM at 1 mM ATP in biochemical assay and approximately 20,000-fold selectivity for PI3Kα, PI3Kβ, PI3Kγ and 57 other kinases.

Sep 01 2021
S8668 GDC-0077 GDC-0077 (RG6114) is a potent selective inhibitor of PI3K alpha (PI3Kα) with an IC50 of 0.038 nM. GDC-0077 is >300-fold more selective for PI3K alpha over the other class I PI3K isoforms (beta, delta, and gamma) and >2000-fold more selective over PIK family members. GDC-0077 binds to the ATP binding site of PI3K and inhibits the phosphorylation of PIP2 to PIP3. Aug 03 2021
S8779 Parsaclisib (INCB050465) Hydrochloride Parsaclisib (INCB050465, IBI376) Hydrochloride is a potent and highly selective PI3Kδ(PI3K delta) inhibitor with an IC50 of 1 nM at 1 mM ATP in biochemical assay and approximately 20,000-fold selectivity for PI3Kα, PI3Kβ, PI3Kγ and 57 other kinases. Jul 23 2021
S9860 BC1618 BC1618 is an orally active Fbxo48 inhibitor that stimulates adenosine monophosphate (AMP)-activated protein kinase (Ampk)-dependent signaling. BC1618 promotes mitochondrial fission, facilitates autophagy and improves hepatic insulin sensitivity. May 24 2021
S6085 KY19382 (A3051) KY19382 (A3051) is a Wnt/β-catenin signalling activator through inhibitory effects on both CXXC5–DVL interaction and GSK3β activity with IC50s of 19 nM and 10 nM, respectively. May 08 2021
S9864 Elimusertib (BAY-1895344) Elimusertib (BAY-1895344) is a very potent and highly selective ATR (ataxia telangiectasia and Rad3-related) inhibitor with IC50 of 7 nM. Elimusertib potently inhibits proliferation of a broad spectrum of human tumor cell lines with median IC50 of 78 nM. Apr 27 2021
S5978 Gallein Gallein (Pyrogallol phthalein) is an inhibitor of G protein βγ (G beta-gamma complex, Gβγ) subunit interaction with PI3 kinase. Gallein inhibits β-ionone effects and exhibits anti-tumor activity. Gallein can be used as a biological stain. Apr 27 2021
S9638 BRD0705 BRD0705 is a potent, paralog selective and orally active inhibitor of GSK3α (Glycogen synthase kinase 3α) with IC50 of 66 nM and Kd of 4.8 μM. BRD0705 also inhibits GSK3β with IC50 of 515 nM. BRD0705 can be used for acute myeloid leukemia (AML). Apr 21 2021
S4572 Homosalate Homosalate (HMS, Homomenthyl salicylate) is an organic ultraviolet filter used in most sunscreens but has been reported to be toxic to marine organisms. Homosalate aggravates the invasion of human trophoblast cells as well as regulates intracellular signaling pathways including PI3K/AKT and MAPK pathways. Mar 30 2021
S7586 PS-48 PS-48 is an allosteric activator of phosphoinositide-dependent protein kinase-1 (PDK1). Mar 30 2021
JAK/STAT
Catalog No. Product Name Information Added
S3566 Cerdulatinib (PRT062070) Cerdulatinib (PRT062070, PRT2070) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM. Mar 04 2021
S9676 PF-06826647 PF-06826647 (Tyk2-IN-8, compound 10) is a selective and orally administered inhibitor of tyrosine kinase 2 (TYK2) with IC50 of 17 nM for binding to TYK2 catalytically active JH1 domain. PF-06826647 (Tyk2-IN-8, compound 10) also inhibits JAK1 and JAK2 with IC50 of 383 nM and 74 nM, respectively. PF-06826647 (Tyk2-IN-8, compound 10) is used in the treatment of psoriasis (PSO). Aug 27 2020
S9664 Colivelin Colivelin (CLN) is a brain-penetrant neuroprotective peptide with potent long-term capacity against deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin is an activator of STAT3. Aug 20 2020
S0918 Ginkgolic acid C17:1 Ginkgolic acid C17:1 (GAC 17:1) inhibits constitutive activation of STAT3 through the abrogation of upstream JAK2 and Src. Ginkgolic acid C17:1 can induce the substantial expression of PTEN and SHP-1. Ginkgolic acid C17:1 induces apoptosis of tumor cells. Jul 26 2020
S0981 BD750 BD750 is an immunosuppressant and a dual inhibitor of JAK3 and STAT5 that inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation with IC50 of 1.5 μM and 1.1 μM for mouse and human T-cell proliferation, respectively. Jul 26 2020
S0818 STAT3-IN-1 STAT3-IN-1 (compound 7d) is an excellent, selective and orally active inhibitor of STAT3 with IC50 of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 induces apoptosis of tumor cells. Jun 05 2020
S1050 TCS PIM-1 1 TCS PIM-1 1 (SC 204330) is a potent and selective inhibitor of ATP-competitive Pim-1 kianse with IC50 of 50 nM, shows good selectivity over Pim-2 and MEK1/MEK2 with IC50 > 20000 nM. May 07 2020
S0437 SAR-20347 SAR-20347 is a potent inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC50 of 0.6 nM, 23 nM, 26 nM and 41 nM, respectively. SAR-20347 inhibits TYK2- and JAK1-mediated IL-12 and IFN-α signaling. Apr 22 2020
S0374 GDC046 GDC046 (Compound 3) is a potent, selective, and orally bioavailable inhibitor of TYK2 with Ki of 4.8 nM, 83.8 nM, 27.6 nM and 253 nM for TYK2, JAK1, JAK2, and JAK3, respectively. Apr 20 2020
S0384 RO495 RO495 (CS-2667) is a potent inhibitor of Non-receptor tyrosine-protein kinase 2 (TYK2). Apr 20 2020
Cell Cycle
Catalog No. Product Name Information Added
S6385 Prexasertib (LY2606368)

Prexasertib (LY2606368, ACR 368) is a selective ATP competitor inhibitor of Chk1 and Chk2 with IC50s of 1 nM and 8 nM in cell-free assays, respectively. Prexasertib also inhibits RSK1 with an IC50 of 9 nM in cell-free assay.

Sep 23 2021
S7837 Centrinone (LCR-263) Centrinone (LCR-263) is a selective and reversible polo-like kinase 4 (PLK4) inhibitor with Ki of 0.16 nM. Jul 23 2021
S6884 LY3405105 LY3405105 is an orally active CDK7 inhibitor with an IC50 of 92.8 nM. LY3405105 shows potential antineoplastic activity. Jul 15 2021
S6875 CASIN CASIN (Pirl1-related Compound 2) directly inhibits activation of Cdc42/RhoGDI with IC50 of 2 μM. Jul 06 2021
S8911 BOS172722 BOS-172722 is a monopolar spindle 1 (MPS1) checkpoint inhibitor with IC50 of 2 nM. Jul 05 2021
S9859 BSJ-4-116 BSJ-4-116 is a specific degrader of cyclin-dependent kinase 12 (CDK12). BSJ-4-116 exhibits potent antiproliferative effects. Jun 21 2021
S9880 MS140 MS140 is a specific and highly potent CDK4/6 kinase inhibitor and also a CDK4/6 degrader (PROTAC). Jun 21 2021
S6768 CC-671 CC-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. Jun 18 2021
S6214 H-1152 dihydrochloride H-1152 dihydrochloride (2HCl) is a membrane-permeable and selective inhibitor of Rho-associated protein kinase (ROCK). H-1152 inhibits ROCK2, PKA, PKC, PKG, AuroraA and CaMK2 with IC50 of 0.0120 μM, 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively. May 31 2021
S9871 BTYNB BTYNB (BTYNB IMP1 Inhibitor, MDK6620) is a potent and selective inhibitor of IMP1 binding to c-Myc mRNA. BTYNB downregulates β-TrCP1 mRNA and reduces activation of nuclear transcriptional factors-kappa B (NF-κB). BTYNB disrupts this enhancer function by impairing IGF2 mRNA-binding protein 1 (IGF2BP1)-RNA association. May 24 2021
DNA Damage
Catalog No. Product Name Information Added
S9903 NRD167

NRD167 is a potent and selective SIRT5 inhibitor.

Sep 10 2021
S6997 CHAPS CHAPS is a zwitterionic surfactant that decreases the sequence specificity of the nucleosome. Apr 27 2021
S5026 Irinotecan hydrochloride Irinotecan (CPT-11, (+)-Irinotecan) hydrochloride is an inhibitor of Topoisomerase I (Topo I) that exhibits cytotoxicity in LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively. Apr 21 2021
S5195 Rucaparib Camsylate Rucaparib (Rubraca, AG014699, PF01367338) Camsylate is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. Apr 21 2021
S4447 Pipobroman Pipobroman (PB, Vercyte), a neutral amide of piperazine, acts as an alkylating agent with antiproliferative activity. Apr 13 2021
S5964 Gatifloxacin hydrochloride Gatifloxacin (AM-1155, CG5501, BMS-206584, PD135432) hydrochloride is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin hydrochloride inhibits bacterial type II topoisomerases with IC50 of 13.8 μg/ml and 0.109 μg/ml for S. aureus topoisomerase IV and E. coli DNA gyrase, respectively. Apr 13 2021
S4948 Rucaparib Rucaparib (Rubraca, AG014699, PF01367338) is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. Apr 07 2021
S3592 4-Phenylbutyric acid (4-PBA) 4-Phenylbutyric acid (4-PBA, Benzenebutyric acid) is a histone deacetylase (HDAC) inhibitor and a key epigenetic inducer of anti-HCV hepatic hepcidin. 4-Phenylbutyric acid inhibits LPS-induced inflammation through regulating endoplasmic-reticulum (ER) stress and autophagy in acute lung injury models. Mar 22 2021
S4476 PCNA-I1 PCNA-I1 is a selective inhibitor of proliferating cell nuclear antigen (PCNA, a potential anticancer target). PCNA-I1 selectively binds to PCNA trimers with Kd of ~0.2 to 0.4 μM. PCNA-I1 inhibits the growth of tumor cells of various tissue types with IC50 of ~0.2 μM. PCNA-I1 induces DNA damage and apoptosis in both LNCaP and PC-3 cells. PCNA-I1 also induces autophagy in PC-3 cells. Mar 19 2021
S3549 PFM01 PFM01, a cell-permeable N-alkylated Mirin derivative, is a selective inhibitor of MRE11 endonuclease activity. Feb 25 2021
TGF-beta/smad
Catalog No. Product Name Information Added
S7692 A-83-01 A-83-01 is a potent inhibitor of TGF-β type I receptor (ALK5-TD) with IC50 of 12 nM. A-83-01 also inhibits the transcription induced by activin/nodal type I receptor (ALK4-TD) and nodal type I receptor (ALK7-TD) with IC50 of 45 nM and 7.5 nM, respectively.Solutions are best fresh-prepared. Jun 03 2020
S0523 SB 4 (Eticovo) SB 4 (Eticovo) is a potent and selective agonist of bone morphogenetic protein 4 (BMP4) signaling with EC50 of 74 nM. SB 4 (Eticovo) enhances canonical BMP signaling and activates SMAD-1/5/9 phosphorylation. Apr 22 2020
S0153 SJ000291942 SJ000291942 is a canonical bone morphogenetic proteins (BMP) signaling pathway activator. Apr 15 2020
S0069 VTX-27 VTX-27 (Compound 27) is a potent and selective inhibitor of protein kinase C θ (PKC θ) with Ki of 0.08 nM and 16 nM for PKC θ and PKC δ, respectively. Apr 13 2020
S2234 BIBF-0775 BIBF-0775 is a selective inhibitor of transforming growth factor β Receptor I (TGFβRI,Alk5) with an IC50 of 34nM. Mar 04 2020
S6654 SRI-011381 SRI-011381 is a novel agonist of the TGF-beta signaling pathway for treatment of Alzheimer's disease. Jan 08 2020
S9522 Valrubicin Valrubicin is a chemotherapy drug used to treat bladder cancer. Valrubicin is a chemotherapy agent, inhibits TPA- and PDBu-induced PKC activation with IC50s of 0.85 and 1.25 μM, respectively. Dec 18 2019
S6713 ITD-1 ITD-1 is a potent TGF-β inhibitor. It does not block the kinase activity of either type I (TGFBR1) or type II (TGFBR2) TGFβ receptors but potently blocks phosphorylation of the effector SMAD2/3 proteins induced by TGFβ2, and only minimally in response to Activin A. Nov 06 2019
S8772 LY 3200882 LY 3200882 is a potent, highly selective inhibitor of TGF-β receptor type 1 (TGFβRI). It potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumor and immune cells and in vivo in subcutaneous tumors in a dose dependent fashion. Jan 09 2019
S8700 TP0427736 HCl TP0427736 is a potent inhibitor of ALK5 kinase activity with an IC50 of 2.72 nM and this effect is 300-fold higher than the inhibitory effect on ALK3 (IC50 = 836 nM for ALK3). It also inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM. Sep 27 2018
GPCR & G Protein
Catalog No. Product Name Information Added
E0039 A-779

A-779 is a potent and selective antagonist for Angiotensin-(1–7) (Ang-(1-7)) with an IC50 of 0.3 nM in a radioligand binding assay. A-779 shows no significant affinity for AT1 or AT2 receptors at a concentration of 1 μM.

Sep 23 2021
E0014 BIBO 3304 Trifluoroacetate

BIBO 3304 Trifluoroacetate (BIBO-3304 TFA) is a novel neuropeptide Y Y1 receptor (NPY1R) antagonist with IC50 values of 0.38 nM and 0.72 nM for human Y1 receptor and rat Y1 receptor, respectively. BIBO 3304 shows low affinity for the human Y2 receptor, human and rat Y4 receptor as well as for the human and rat Y5 receptor (IC50 values >1000 nM).

Sep 10 2021
E0013 DAMGO

DAMGO (DAGO) is a potent and selective μ opioid receptor agonist with ki of 17 nM.

Sep 10 2021
E0021 Apraglutide (FE 203799)

Apraglutide (FE 203799) is a potent and highly selective GLP-2 agonist with EC50s of 0.03 nM and 0.07 nM for hGLP-2 Receptor and rGLP-2 Receptor, respectively.

Sep 10 2021
S9935 Teduglutide Teduglutide (ALX-0600, Gattex, Revestive, TAK 633) is an analogue of human glucagon-like peptide-2 (GLP-2) and binds to the GLP-2 receptors. Teduglutide prolongs the intestinotrophic properties of GLP-2 in animal models. Aug 19 2021
S9915 FSLLRY-NH2 TFA FSLLRY-NH2 TFA (FSY-NH2) is a selective protease-activated receptor 2 (PAR2) inhibitor with an ic50 of 50 µM in PAR2-KNRK cells. Aug 11 2021
S9477 AH7614 AH7614 (compound 39) is a selective FFA4 (GPR120) antagonist with pIC50s of 7.1 for human FFA4 and 8.1 for mouse FFA4. Aug 11 2021
S6981 Glycerol phenylbutyrate Glycerol phenylbutyrate (GT4P, HPN-100M, Ravicti) is a nitrogen-binding agent and acts as a sigma-2 (σ2) receptor ligand with a pKi of 8.02. Glycerol phenylbutyrate is a prodrug in which phenylbutyrate (PBA) is released from the glycerol backbone by lipases in the gastrointestinal tract. Jul 16 2021
P1203 Avexitide Avexitide (Exendin (9-39)) is a specific and competitive antagonist of glucagon-like peptide-1 (GLP-1) receptor. Jun 07 2021
S6347 5'-N-Ethylcarboxamidoadenosine (NECA) 5'-N-Ethylcarboxamidoadenosine (NECA, 5'-(N-Ethylcarboxamido)adenosine, Adenosine-5'N-ethylcarboxamide, 5'-Ethylcarboxamidoadenosine) is a stable, nonselective adenosine receptor agonist. 5'-N-Ethylcarboxamidoadenosine acts via multiple mechanisms including: reducing diabetes-induced oxidative stress, inhibiting gene expression of IL-18, TNF-α and ICAM-1 (intercellular adhesion molecule 1 (CD54)), and blocking activation of the JNK-MAPK pathway. Jun 07 2021
PTK
Catalog No. Product Name Information Added
S7647 Lucitanib (E3810) hydrochloride Lucitanib (E-3810, AL3810) hydrochloride is a dual inhibitor of Vascular endothelial growth factor receptor (VEGFR) and Fibroblast growth factor receptor (FGFR). Lucitanib hydrochloride (E-3810, AL3810) potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50 of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively. Jun 28 2021
S6515 ALW II-41-27 ALW II-41-27 (compound 7) is a potent inhibitor of Eph receptor tyrosine kinase with Kd of 12 nM for EphA2. May 06 2021
S4967 Ceritinib dihydrochloride Ceritinib (Zykadia, LDK378) dihydrochloride is a selective, orally bioavailable and ATP-competitive inhibitor of ALK with IC50 of 0.2 nM. Ceritinib dihydrochloride also inhibits InsR, IGF-1R and STK22D with IC50 of 7 nM, 8 nM and 23 nM, respectively. Ceritinib exhibits antitomor activity. Apr 21 2021
S5190 Crizotinib hydrochloride Crizotinib (PF-02341066) hydrochloride (Xalkori) inhibits tyrosine phosphorylation of c-Met and nucleophosmin (NPM)-anaplastic lymphoma kinase (ALK) with IC50 of of 11 nM and 24 nM in cell-based assays, respectively. Crizotinib hydrochloride is also a potent ROS1 inhibitor with Ki less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines. Apr 21 2021
S4947 Regorafenib Hydrochloride Regorafenib (Stivarga, BAY 73-4506) Hydrochloride is a multi-target inhibitor for VEGFR1, Murine VEGFR2/3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM, 4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively. Apr 13 2021
S9711 CH7233163 CH7233163 is a non-covalent ATP competitive inhibitor of EGFR-tyrosine kinase with antitumor activities against tumor with EGFR-Del19/T790M/C797S. Apr 07 2021
S9786 BDTX-189 BDTX-189 is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations with Kd of 0.2 nM, 0.76 nM, 13 nM and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. BDTX-189 exhibits anticancer activity. Mar 15 2021
S6839 MRX-2843 MRX-2843 (UNC2371) is an orally active dual inhibitor of tyrosine kinases MERTK and FLT3 with IC50 of 1.3 nM and 0.64 nM, respectively. Feb 08 2021
S5860 Larotrectinib Larotrectinib (Vitrakvi, LOXO-101, ARRY-470) is an ATP-competitive, oral administered and highly selective inhibitor of the tropomyosin-related kinase (TRK) family receptors. Feb 08 2021
S3187 SBI-477 SBI-477 is an insulin signaling inhibitor that deactivates the transcription factor MondoA, leading to reduced expression of the insulin pathway suppressors thioredoxin-interacting protein (TXNIP) and arrestin domain-containing 4 (ARRDC4). SBI-477 inhibits triacylglyceride (TAG) synthesis and enhances basal glucose uptake in human skeletal myocytes. Dec 24 2020
Epigenetics
Catalog No. Product Name Information Added
S8996 SNDX-5613 SNDX-5613 is a potent and selective inhibitor of menin-MLL binding with a Ki of 0.15 nM. SNDX-5613 shows anti-proliferative activity against multiple cell lines harboring MLLr translocations (MV4;11, RS4;11, MOLM-13, KOPN-8) with IC50 values ranging from 10-20 nM. Jul 16 2021
S9691 BMS-986158 BMS-986158 is a potent inhibitor of BET with IC50s of 6.6 nM and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respectively. Jul 15 2021
S9805 WM-3835 WM-3835 is a novel and high-specific small molecule Lysine Acetyltransferase 7 (KAT7, MYST2, HBO1) inhibitor, able to potently suppressed OS cell proliferation and migration, and leads to apoptosis activation. Jun 28 2021
S9667 CCS-1477 (CBP-IN-1) CCS1477(CBP-IN-1, CBP/p300-IN-4)is a potent and selective inhibitor of p300/CBP bromodomain. CCS1477 works by inhibiting the expression and function of the androgen receptor (AR), as well as inhibiting c-Myc. Apr 27 2021
S9685 GSK620 GSK620 is a pan-BD2 inhibitor, which shows an anti-inflammatory phenotype in human whole blood with excellent broad selectivity, developability, and in vivo oral pharmacokinetics. Mar 30 2021
S3573 CC-90010 CC-90010 is a reversible, orally active and central nervous system-penetrant inhibitor of bromodomain and extra-terminal (BET) proteins. CC-90010 is applied in the study for advanced solid tumors. Mar 04 2021
S8665 GNE-781 GNE-781 (compound 19) is an orally active, highly potent and selective bromodomain inhibitor of cyclic adenosine monophosphate response element binding protein (CBP) with IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50 of 6.2 nM and 5100 nM, respectively. GNE-781 exhibits antitumor activity. Jan 25 2021
S1161 Histone Acetyltransferase Inhibitor II

Histone Acetyltransferase Inhibitor II (HAT Inhibitor II, compound 2c) is a potent, selective and cell-permeable p300 histone acetyltransferase (HAT) inhibitor with IC50 of 5 μM. Histone Acetyltransferase Inhibitor II shows anti-acetylase activity in mammalian cells.

Nov 27 2020
S1325 L-2-Hydroxyglutaric acid disodium

L-2-Hydroxyglutaric acid disodium ((S)-2-Hydroxyglutaric acid disodium, L-2-Hydroxyglutarate disodium, LGA, L-2HG) is an epigenetic modifier and a putative oncometabolite in kidney cancer that inhibits histone demethylases and hence promotes histone methylation. L-2-Hydroxyglutaric acid disodium is also an inhibitor of mitochondrial creatine kinase (Mi-CK) with Km and Ki of 2.52 mM and 11.13 mM, respectively.

Nov 23 2020
S1242 CPTH2 CPTH2 is a potent histone acetyltransferase (HAT) inhibitor modulating Gcn5p network. CPTH2 induces apoptosis and decreases the invasiveness of a ccRCC cell line through the inhibition of KAT3B. Nov 18 2020
NF-κB
Catalog No. Product Name Information Added
S5899 (R)-(-)-Ibuprofen (R)-(-)-Ibuprofen ((R)-Ibuprofen) inhibits the activation of NF-κB in response to T-cell stimulation with IC50 of 121.8 μM. R(-)-ibuprofen exerts anti-inflammatory and antinociceptive effects. May 06 2021
S4611 TCEP Hydrochloride TCEP (Tris(2-carboxyethyl)phosphine) hydrochloride, a non-thiol reducing agent, promotes NF-κB-DNA binding in a dose-related manner. Apr 07 2021
S3384 (E/Z)-IT-603 (E/Z)-IT-603 is a mixture of E-IT-603 and Z-IT-603. IT-603 is a NF-κB family member c-Rel inhibitor with an IC50 of 3 μM in electrophoretic mobility shift assay (EMSA). Dec 11 2020
S1321 Urolithin B Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα. Urolithin B suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass. Nov 18 2020
S8922 TBK1/IKKε-IN-1(compound 1) TBK1/IKKε-IN-1 (compound 1) is a dual inhibitor of TANK-binding kinase 1 (TBK1) and IκB kinase-ε (IKKε/IKK-i) with IC50 of 1.0 nM and 5.6 nM for TBK1 and IKKε, respectively. TBK1/IKKε inhibition enhances response to PD-1 blockade, which effectively predicts tumor response in vivo. May 14 2020
S0507 CBL0137 CBL0137 (Curaxin-137) is an inhibitor of the histone chaperone FACT (facilitates chromatin transcription) that simultaneously suppresses NF-κB and activates p53 with EC50 of 0.47 μM and 0.37 μM, respectively. Apr 22 2020
S0425 TBK1/IKKε-IN-2 TBK1/IKKε-IN-2 (Ikk epsilon-in-1, IKKε-IN-1, MDK10496) is a dual inhibitor of TBK1 and IKKε. Apr 22 2020
S6671 SN50 SN50 (NF-κB SN50), a cell-permeable NF-κB inhibitory peptide, is composed of the signal peptide of Kaposi fibroblast growth factor.SN50 inhibits the activation of NF-κB and attenuates ventilator-induced lung injury. Mar 25 2020
S8935 BAY-985 BAY-985 is a potent and highly selective TBK1/IKKε inhibitor. BAY-985 shows high potency toward TBK1 (IC50 = 2 nM, low ATP assay; 30 nM, high ATP assay) and IKKε(IC50 = 2 nM), as well as high potency in the mechanistic pIRF3 assay (IC50 = 74 nM), and an antiproliferative effect on SK-MEL-2 cells (IC50 = 900 nM). Mar 25 2020
S8941 NIK SMI1 NIK SMI1 is a highly potent and selective NF-κB-inducing kinase (NIK) inhibitor with Ki of 0.23 nM for NIK-catalyzed hydrolysis of ATP to ADP. Mar 25 2020
Metabolism
Catalog No. Product Name Information Added
S9706 OT-82 OT-82 is a novel nicotinamide phosphoribosyltransferase (NAMPT) inhibitor with average IC50s of 13.03   nM in non-HP cancer cells and 2.89   nM in HP cancer cells, respectively. Sep 16 2021
S9914 CITCO

CITCO is a potent and selective constitutive androstane receptor (CAR) agonist with EC50 of 49 nM. CITCO displays >50-fold selectivity for CAR over PXR in the transient transfection assay.

Sep 16 2021
S9606 Galloflavin Galloflavin (NSC 107022) is a novel inhibitor of lactate dehydrogenasee (LDH) with Ki values of 5.46 μM and 15.06 μM for LDH-A and LDH-B, respectively. Sep 16 2021
E0032 Olesoxime (TRO 19622)

Olesoxime (TRO19622) is a novel, orally active and CNS-penetrant mitochondrial-targeted neuroprotective compound.

Sep 01 2021
S6388 SHP099 SHP099 is a highly potent, selective and orally bioavailable small-molecule SHP2 inhibitor with an IC50  value of  71 nM and shows no activity against SHP1. Jul 28 2021
S9478 Trans-4-Phenyl-3-buten-2-one Trans-4-Phenyl-3-buten-2-one (trans-Benzylideneacetone, trans-Benzalacetone, trans-Benzylideneacetone) is an inhibitor of the enzyme phospholipase A2 (PLA2). Trans-4-Phenyl-3-buten-2-one is used as a flavouring agent, a fragrance and a bacterial metabolite. Jul 23 2021
S6895 TCPOBOP TCPOBOP is a constitutive androstane receptor (CAR) agonist. TCPOBOP attenuates Fas-induced murine liver injury by altering Bcl-2 proteins. Jul 06 2021
S6391 Sephin-1 Sephin-1 (NSC-65390) is a selective inhibitor of a holophosphatase, a small molecule that safely and selectively inhibits a regulatory subunit of protein phosphatase 1 in vivo. Sephin-1 (NSC-65390) selectively bounds and inhibits the stress-induced PPP1R15A. Jul 05 2021
S9776 AG-636 AG-636 is an orally available inhibitor of dihydroorotate dehydrogenase (DHODH) with potential antineoplastic activity. Jun 28 2021
S6971 Ervogastat Ervogastat (PF-06865571, DGAT2i) is a potent diacylglycerol acyltransferase 2 (DGAT2) inhibitor that reduces steatosis and hepatic triglyceride levels in non-alcoholic steatohepatitis (NASH). Jun 25 2021
Proteases
Catalog No. Product Name Information Added
S9896 JNJ-67856633

JNJ-67856633 (JNJ-6633) is a potent, selective, allosteric inhibitor of MALT1 protease.

Sep 23 2021
S9909 ARP 100 ARP 100 (MMP-2 Inhibitor III, Compound 10a) is a potent and selective inhibitor of MMP-2 with an IC50 of 12 nM and displays less inhibitory activity at MMP-9, MMP-3, MMP-1 and MMP-7 with IC50s of 200 nM, 4500 nM, >50,000 nM and >50,000 nM respectively. Sep 01 2021
S5960 Dabigatran etexilate mesylate Dabigatran etexilate mesylate (Pradaxa, BIBR 1048MS, Dabigatran etexilate methanesulfonate) is an orally active prodrug of Dabigatran which is a reversible and selective, direct thrombin inhibitor (DTI). Dabigatran selectively and reversibly inhibits human thrombin with Ki of 4.5 nM and thrombin-induced platelet aggregation with IC50 of 10 nM. Apr 27 2021
S4432 Ixazomib Citrate (MLN9708) Ixazomib citrate (MLN9708, Ninlaro) is a prodrug of Ixazomib (MLN2238), which is a selective, orally bioavailable inhibitor of 20S proteasome that inhibits the chymotrypsin-like proteolytic (β5) site with IC50 of 3.4 nM and Ki of 0.93 nM, respectively. Ixazomib (MLN2238) also inhibits caspase-like (β1) and trypsin-like (β2) proteolytic sites with IC50 of 31 nM and 3500 nM, respectively. Apr 13 2021
S4426 Sacubitril hemicalcium salt Sacubitril (AHU-377) hemicalcium salt, a component of the heart failure medicine LCZ696, is a potent inhibitor of neprilysin (neutral endopeptidase, NEP). Mar 30 2021
S0479 ZK824859 ZK824859 is a potent, selective and orally bioavailable inhibitor of urokinase plasminogen activator (uPA) with IC50 of 79 nM, 1580 nM and 1330 nM for human uPA, tPA, and plasmin, respectively. Feb 22 2021
S3511 FOY251 FOY251, an active metabolite of camostat mesilate, is an inhibitor of synthetic serine protease. FOY251 inhibits SARS-CoV-2 infection. Jan 28 2021
S3388 Sacubitrilat Sacubitrilat (Sac, LBQ-657) is an active inhibitor of neprilysin (NEP). Dec 11 2020
S3395 Tegobuvir Tegobuvir (TGV, GS 333126, GS-9190) is a non-nucleoside inhibitor of HCV RNA replication with proven antiviral activity in HCV-infected patients. Dec 11 2020
S2985 N-Acetyl-5-hydroxytryptamine

N-Acetyl-5-hydroxytryptamine (NAS, N-Acetylserotonin, Normelatonin, O-Demethylmelatonin), a precursor of melatonin, is a potent and selective agonist of TrkB receptor.

Dec 07 2020
Microbiology
Catalog No. Product Name Information Added
E0005 Enfuvirtide Acetate Enfuvirtide Acetate (T20 Acetate, DP178 Acetate) is an HIV fusion inhibitor with ic50s of 13.63  nM and 30.21  nM on infection by HIV-1IIIB in MT-2 cells and HIV-1Bal in M7 cells, respectively. Aug 11 2021
S6090 JFD01307SC JFD01307SC ([(1,1-dioxidotetrahydrothien-3-yl)amino]acetic acid) shows activity against M.tuberculosis with minimum inhibitory concentrations (MICs) in the range of 8 to 16 µg/ml. JFD01307SC may targets enzymes involved in glutamine biosynthesis. May 08 2021
S5235 Cefodizime Cefodizime (CEF, CDZ) is an aminothiazolyl cephalosporin with a broad spectrum of antibacterial activity. Apr 27 2021
S5979 2',3'-Dideoxyadenosine 2',3'-Dideoxyadenosine (ddA, ddAdo) is an anti-human immunodeficiency virus agent against human immunodeficiency virus (HIV) and human hepatitis B virus (HBV) replication. Apr 27 2021
S5330 Amikacin Sulfate Salt Amikacin (BAY 41-6551) sulfate, a semisynthetic analog of kanamycin, is an aminoglycoside antibiotic which is very active against most gram-negative bacteria including gentamicin- and tobramycin-resistant strains. Apr 27 2021
S5961 Prednisolone disodium phosphate Prednisolone disodium phosphate (Hydeltrasol, Prednisolone 21-phosphate disodium) is a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties that exerts late mitogenic and biphasic effects on resistant acute lymphoblastic leukemia cells. Apr 27 2021
S5080 Neticonazole Neticonazole (SS717) is a selecvie inhibitor of exosome biogenesis and secretion. Neticonazole exhibits Neticonazole antifungal and antitumor activity. Apr 21 2021
S4974 Oxacillin sodium Oxacillin sodium (salt) is a narrow-spectrum β-lactam antibiotic that can be used for treatment of methicillin-sensitive Staphylococcus aureus (MSSA) bacteremia. Apr 13 2021
S5186 Cefpiramide Cefpiramide (Cefpiramide acid, Cefpiramido, Cefpiramidum, WY-44635, SM-1652) is a pseudomonas-active cephalosporin with a broad spectrum of antibacterial activity. Apr 13 2021
S5008 Ciprofloxacin hydrochloride Ciprofloxacin (CPX, Cetraxal, Ciloxan, Cipro, Bay-09867) hydrochloride, a fluorinated quinolone, is a β-diketone antibiotic with a broad spectrum antibacterial activity. Ciprofloxacin is an inhibitor of bacterial DNA gyrase (a subclass of Type II topoisomerases). Apr 13 2021
Apoptosis
Catalog No. Product Name Information Added
S6709 Obatoclax (GX15-070)

Obatoclax (GX15-070) is an antagonist of Bcl-2 with an Ki of 0.22 μM in a cell-free assay, can assist in overcoming MCL-1 mediated resistance to apoptosis.

Sep 10 2021
S9705 Apostatin-1 Apostatin-1 (Apt-1) is a novel TRADD inhibitor. Apostatin-1 binds to a pocket on the N-terminal TRAF2-binding domain of TRADD (TRADD-N). Apostatin-1 inhibits bortezomib-induced apoptosis and RIPK1-dependent apoptosis (RDA) with an IC50 of about 1 μM. Sep 01 2021
E0035 CP-31398 Dihydrochloride

CP-31398 Dihydrochloride stabilizes the active conformation of p53 and promotes p53 activity in cancer cell lines with mutant or wild-type p53.

Sep 01 2021
S9726 Rimiducid (AP1903) Rimiducid (AP1903) is a chemical protein dimerizer and binds tightly to the target FKBP fusion protein while binding minimally to the abundant natural FKBP. Rimiducid elicites potent and dose-dependent apoptosis of cells in culture expressing dimerizer-dependent Fas constructs, with an EC50 of ≈0.1 nM. Aug 23 2021
S9840 SRS16-86 SRS16-86, a novel third-generation ferrostatin, is an inhibitor of ferroptosis. Jun 07 2021
S9733 Mito-TEMPO Mito-TEMPO (MT), a mitochondria-targeted superoxide dismutase mimetic, protects against the early phase of acetaminophen (APAP) hepatotoxicity by inhibiting peroxynitrite formation. Mito-TEMPO treatment inhibits APAP-induced RIP3 kinase expression. Jun 07 2021
S9839 SRS11-92 SRS11-92 (AA9), a Ferrostatin-1 (Fer-1) analogue, is a potent inhibitor of ferroptosis. SRS11-92 inhibits ferroptotic cell death induced by Erastin in HT-1080 human fibrosarcoma cells with EC50 of 6 nM. Jun 07 2021
S9817 Ac-FLTD-CMK Ac-FLTD-CMK is a specific inhibitor for inflammatory caspases. Ac-FLTD-CMK inhibits gasdermin D (GSDMD) cleavage by caspases-1, -4, -5, and -11 in vitro. Ac-FLTD-CMK is effective against caspases-1, caspases-4 and caspases-5 with IC50 of 46.7 nM, 1.49 μM and 329 nM, respectively. May 31 2021
S4613 Sodium Fluoride Sodium fluoride (NaF) induces apoptosis and autophagy via the endoplasmic reticulum (ER) stress pathway in MC3T3-E1 osteoblastic cells. May 09 2021
S6078 ICCB-19 hydrochloride ICCB-19 hydrochloride is an inhibitor of TNFRSF1A Associated Via Death Domain (TRADD) with IC50 of 1.12 μM and 2.01 μM for protecting Velcade-induced apoptosis in Jurkat cells and protecting RDA in MEFs, respectively. ICCB-19 indirectly inhibits Receptor-interacting serine/threonine-protein kinase 1 (RIPK1). ICCB-19 effectively induces autophagy. May 08 2021
MAPK
Catalog No. Product Name Information Added
S4484 Trametinib DMSO solvate Trametinib (GSK1120212, JTP-74057, Mekinist) DMSO solvate is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assay. Trametinib activates autophagy and induces apoptosis. Apr 07 2021
S8569 KO-947 KO-947 is a potent and selective inhibitor of ERK1/2 kinases. KO-947 blocks ERK signaling and proliferation of tumor cells exhibiting dysregulation of MAPK pathway signaling at low nanomolar concentrations. Dec 07 2020
S6905 MCP110 MCP110 is an inhibitor of Ras/Raf-1 interaction. MCP110 disrupts the interaction of activated Ras with Raf and is potential for the treatment of human tumors. Sep 24 2020
S6888 SEL201 SEL-201 (SLV-2436, SEL201-88) is a highly potent and ATP-competitive inhibitor of MNK1 and MNK2 with IC50 of 10.8  nM and 5.4 nM, respectively. Sep 10 2020
S6882 HI-TOPK-032 HI-TOPK-032 is a potent and specific inhibitor of TOPK. HI-TOPK-032 also reduces ERK-RSK phosphorylation, regulates of the abundance of p53, cleaved caspase-7, and cleaved PARP, and induces apoptosis in cancer cells. Aug 06 2020
S8896 BAY-885 BAY-885 is a highly potent and selective ERK5 inhibitor. Jul 05 2020
S7794 JNK Inhibitor VIII JNK Inhibitor VIII (TCS JNK 6o) is an inhibitor of c-Jun N-terminal kinases with IC50 of 45 nM and 160 nM for JNK-1 and JNK-2, respectively. JNK Inhibitor VIII (TCS JNK 6o) inihibits JNK-1, JNK-2, and JNK-3 with Ki of 2 nM, 4 nM and 52 nM, respectively. Jul 01 2020
S8900 SR18662 SR18662 is an optimized compund based on ML264 that inhibits Krüppel-like factor 5 (KLF5) with IC50 of 4.4 nM. SR18662 reduces the viability of multiple colorectal cancer cell lines. SR18662 induces apoptosis. Jul 01 2020
S0872 ASTX-029 ASTX-029 is an orally bioavailable inhibitor of the extracellular signal-regulated kinases (ERK) 1 and 2, with potential antineoplastic activity. ASTX-029 inhibits ERK-dependent tumor cell proliferation and survival. Jun 19 2020
S9621 Donafenib (Sorafenib D3) Donafenib (Sorafenib D3, Bay 43-9006 D3, CM-4307) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 15 nM, 20 nM and 22 nM for Raf-1, mVEGFR-2, mVEGFR-3 and B-RAF, respectively. Jun 19 2020
Angiogenesis
Catalog No. Product Name Information Added
S6383 1-NM-PP1 1-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. Jun 15 2021
S6966 MT-802 MT-802 is a potent PROTAC that induces Bruton's tyrosine kinase (BTK) knockdown. MT-802 recruits BTK to the cereblon E3 ubiquitin ligase complex to trigger BTK ubiquitination and degradation via the proteasome. MT-802 has potential for treatment of C481S mutant chronic lymphocytic leukemia (CLL). May 31 2021
S4895 Nilotinib hydrochloride monohydrate Nilotinib (AMN-107, Tasigna) hydrochloride monohydrate is a selective and orally bioavailable inhibitor of Bcr-Abl with IC50 < 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition. Apr 07 2021
S4944 Fostamatinib disodium hexahydrate Fostamatinib (R788) disodium (Tamatinib Fosdium) hexahydrate, a prodrug of the active metabolite R406, is a Syk inhibitor with IC50 of 41 nM in a cell-free assay. Apr 07 2021
S8948 SRX3207 SRX3207 is an orally active dual inhibitor of Syk-PI3K with IC50 of 39.9 nM, 31200 nM, 3070 nM, 3070 nM, 244 nM, 388 nM, 9790 nM for Syk, Zap70, BRD41, BRD42, PI3K alpha, PI3K delta, PI3K gamma, respectively. SRX3207 blocks tumor immunosuppression and increases anti-tumor immunity. Mar 30 2021
S9715 Lanraplenib (GS-9876) Lanraplenib (GS-9876, GS-SYK) is a potent, highly selective and orally active inhibitor of Spleen Tyrosine Kinase (SYK) with IC50 of 9.5 nM. Lanraplenib inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans. Feb 22 2021
S0908 β,β-Dimethylacrylshikonin β,β-Dimethylacrylshikonin promotes angiogenesis by inducing eNOS, VEGF and HIF-1α expression through the PI3K-dependent pathway. β,β-Dimethylacrylshikonin is a naphthoquinone derivative isolated from Arnebia nobilis. Dec 23 2020
S1232 M1001 M1001 is a weak agonist of hypoxia-inducible factor-2α (HIF-2α) that binds to the HIF-2α PAS-B domain with Kd of 667 nM. Nov 18 2020
S1272 XL228 XL228 is a protein kinase inhibitor with IC50 of 5 nM, 1.4 nM, 3.1 nM, 1.6 nM, 6.1 nM and 2 nM for wild-type ABL kinase, ABL T315I, Aurora A, IGF-1R, SRC and LYN, respectively. Nov 18 2020
S9699 Desidustat Desidustat (ZYAN1, ZYAN1-1001), an antianaemic drug candidate, is an orally active hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) inhibitor (HIF-PHI) that stimulates erythropoiesis. Sep 17 2020
Stem Cell & Wnt
Catalog No. Product Name Information Added
E0033 IWP-4

IWP-4 is a potent Wnt/β-catenin signaling pathway inhibitor with an IC50 of 25 nM.

Sep 01 2021
S5992 Heparan Sulfate Heparan sulfate (HS, Heparitin sulfate, Alpha-idosane, HHS 5, N-Acetylheparan Sulfate, Suleparoid, Tavidan), a constituent of HS proteoglycans (HSPGs), is a linear polysaccharide present on the cell surface. Heparan sulfate influences the binding affinity of intestinal epithelium cells (IECs) to Wnt, thereby promoting activation of canonical Wnt signaling and facilitating regeneration of small intestinal crypts after epithelial injury. May 17 2021
S9828 WAY-262611 WAY-262611 (BML-WN110, Compound 5) is a beta-catenin (β-Catenin) agonist that increases bone formation rate with EC50 of 0.63 μM in TCF-Luciferase assay. WAY-262611 is also an inhibitor of dickkopf 1 (DKK1). May 06 2021
S6961 Foxy-5 Foxy-5, a Wnt-5a mimicking hexapeptide, is a WNT signalling pathway modulator potentially for the treatment of metastatic breast cancer, prostate cancer and colorectal cancer. Jan 11 2021
S2962 NP-G2-044 NP-G2-044 is a potent, orally active inhibitor of the actin-bundling activity of fascin with IC50 of ~0.2 μM. NP-G2-044 blocks tumor metastasis and increases antitumor immune response. Nov 06 2020
S6901 MSAB MSAB is a selective inhibitor of Wnt/β-catenin signaling that binds to β-catenin, promoting its degradation, and specifically downregulates Wnt/β-catenin target genes. MSAB shows potent anti-tumor effects. Sep 03 2020
S8968 PRI-724 PRI-724 (C-82 prodrug, ICG-001 analog) is a potent and specific inhibitor that disrupts the interaction of β-catenin and CBP. Jul 05 2020
S0733 Tegatrabetan (BC-2059) Tegatrabetan (BC2059) is an antagonist of β-Catenin. Tegatrabetan (BC2059) treatment disrupts the binding of β-catenin with the scaffold protein transducin β-like 1 (TBL1) and proteasomal degradation and declines in the nuclear levels of β-catenin. May 09 2020
S7981 CCT251545 CCT251545 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. Apr 26 2020
S0458 KY1220 KY1220 is a small molecule that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway with IC50 of 2.1 μM in HEK293 reporter cells. Apr 22 2020
Ubiquitin
Catalog No. Product Name Information Added
S6943 IU1-47 IU1-47 is a potent and specific inhibitor of USP14 with an IC50 of 0.6 μM. IU1-47 shows ∼33-fold selectivity for USP14 over USP5 (IsoT). Sep 10 2021
S8300 CC-885

CC-885 is a novel cereblon (CRBN) modulator. CC-885 selectively promotes CRBN- and p97-dependent PLK1 ubiquitination and degradation.

Sep 01 2021
S9832 CC-90009 CC-90009 is a novel cereblon (CRBN) E3 ligase modulator and specifically targets GSPT1 (G1 to S phase transition 1) for proteasomal degradation. Aug 19 2021
S6883 HBX 19818 HBX19818 is a specific inhibitor of USP7 with an IC 50 of 28.1 μM. Jul 23 2021
S8967 XL177A XL177A is a potent, selective and irreversible inhibitor of Ubiquitin specific peptidase 7 (USP7) with IC50 of 0.34 nM. May 24 2021
S9724 SZL P1-41 SZL P1-41 (compound #25) is a specific inhibitor of S-phase kinase-associated protein 2 (Skp2) that indeed binds to Skp2, prevents Skp2-Skp1 interaction and inhibits Skp2 SCF E3 ligase activity, which consequently suppresses survival of cancer cells and cancer stem cells. SZL P1-41 causes higher apoptosis rates in cancer cells. Apr 27 2021
S4453 NPD8733 NPD8733 is an inhibitor of cancer cell-enhanced fibroblast migration that specifically binds to valosin-containing protein (VCP)/p97, a member of the ATPase-associated with diverse cellular activities (AAA+) protein family. Mar 19 2021
S3502 (S,R,S)-AHPC-PEG4-NH2 hydrochloride (S,R,S)-AHPC-PEG4-NH2 hydrochloride (VH032-PEG4-NH2 hydrochloride, VHL Ligand-Linker Conjugates 4 hydrochloride, E3 ligase Ligand-Linker Conjugates 7) is a PROTAC E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker. Feb 08 2021
S8697 ML792 ML-792 is a potent and selective inhibitor of SUMO (small ubiquitin-like modifier)-activating enzyme (SAE). ML-792 inhibits SAE/SUMO1 and SAE/SUMO2 in ATP–inorganic pyrophosphate (PPi) exchange assays with IC50 of 3 nM and 11 nM, respectively. Jan 05 2021
S2881 Homo-PROTAC cereblon degrader 1 Homo-PROTAC cereblon degrader 1 (OUN20985) is a potent and efficient cereblon (CRBN) degrader with minimal effects on IKZF1 and IKZF3. Dec 23 2020
Neuronal Signaling
Catalog No. Product Name Information Added
S6985 Varenicline Varenicline is highly selective and blocks more potently to α4β2 receptors than to other common nicotinic receptors (>500-fold α3β4, >3,500-fold α7, >20,000-fold α1βγδ), or to non-nicotinic receptors and transporters (>2,000-fold). Varenicline also acts as an agonist of 5-HT3 serotonine receptors. Jul 26 2021
S6853 ONC206 ONC206 is a selective antagonist of dopamine D2-like receptors (DRD2/3/4) with broad-spectrum anti-tumor activity. May 24 2021
S3913 Pimethixene maleate Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.30, 7.28, 7.61, 6.37, 8.19, 7.54, 10.14, 8.61 and 9.38, respectively. Apr 27 2021
S5770 Pizotifen Pizotifen (Pizotyline, BC-105) is a potent antagonist of 5-Hydroxytryptamine (5-HT, Serotonin) 5-HT2 receptor with a high affinity for 5-HT1C binding site. Apr 27 2021
S9789 JHU37152 JHU37152 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.8 nM and 8.7 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively. Apr 27 2021
S9790 JHU37160 JHU37160 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.9 nM and 3.6 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 18.5 nM and 0.2 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively. Apr 27 2021
S4724 Etomidate hydrochloride Etomidate (Amidate, R 16659) hydrochloride is a general anesthetic that produces its effects by enhancing GABA(A) receptor activity. Apr 21 2021
S5022 Varenicline Hydrochloride Varenicline (CP 526555) Hydrochloride is a potent and selective inhibitor of nicotine acetylcholine receptor (nAChR) with Ki of 0.12 nM and 0.14 nM for α6β2 nAChR and α4β2 nAChR, respectively. Apr 21 2021
S5185 Perospirone Perospirone (SM-9018 free base) is an orally active antagonist of 5-hydroxytryptamine2 (5-HT2) receptor, dopamine2 (D2) receptor and 5-HT1A receptor with Ki of 0.6 nM, 1.4 nM and 2.9 nM, respectively. Apr 21 2021
S5777 Ipratropium bromide monohydrate Ipratropium bromide (Atrovent, Sch 1000) monohydrate is an antagonist of muscarinic acetylcholine receptors (mAChR) with IC50 of 2.9 nM, 2.0 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Apr 21 2021
Others
Catalog No. Product Name Information Added
E0040 Gap 27

Gap 27 is a synthetic connexin-mimetic peptide and acts as a gap junction inhibitor. Gap 27 is highly effective in interrupting co-operative cell-cell interactions, such as the synchronous beating of embryonic cardiomyocytes.

Sep 23 2021
S8912 Eribulin Mesylate (E7389)

Eribulin Mesylate (E7389, B-1939, ER-086526), an analogue of the marine natural product halichondrin B, is a nontaxane completely synthetic microtubule inhibitor.

Sep 23 2021
S9926 ML-SA1

ML-SA1 (Mucolipin synthetic agonist 1) is an activator of TRPML channels. ML-SA1 also inhibits Dengue virus 2 (DENV2) and Zika virus (ZIKV) by promoting lysosomal acidification and protease activity. The IC50 values of ML-SA1 against DENV2 RNA and ZIKV RNA are 8.93 μM and 52.99 μM, respectively. ML-SA1 induces autophagy. ML-SA1 can be used for the research of broad-spectrum antiviral.

Sep 16 2021
E0029 Hexa-D-arginine

Hexa-D-arginine is a potent and specific furin inhibitor with Ki values of 106 nM, 580 nM, and 13.2 μm for furin, PACE4, and PC1, respectively.

Sep 10 2021
E0031 RN-1747

RN-1747 is a selective TRPV4 agonist with EC50s of 0.77 μM, 4.0 μM and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4, respectively. RN-1747 also antagonizes TRPM8 with IC50 of 4 μM.

Sep 10 2021
E0016 Tertiapin-Q

Tertiapin-Q (TPNQ) is a derivative of tertiapin and inhibits BK-type K+ channels in a use- and concentration-dependent manner. Tertiapin-Q also binds to ROMK1 (Kir1.1) and GIRK1/4 (Kir3.1/3.4) channels with Ki values of 1.3 nM and 13.3 nM respectively.

Sep 10 2021
S9903 NRD167

NRD167 is a potent and selective SIRT5 inhibitor.

Sep 10 2021
S9787 Conoidin A

Conoidin A is a covalent inhibitor of peroxiredoxin II with an IC50 of 25.1 mM for recombinant T. gondii enzyme peroxiredoxin II (rTgPrxII).

Sep 01 2021
E0030 NS309

NS309 is a potent and selective activator of human Ca2+ -activated K+ channels of SK and IK types with an EC50 of 150  nM for hSK3 channel, and displays no activity at BK channels.

Sep 01 2021
E0028 9-Phenanthrol

9-Phenanthrol (9-Hydroxyphenanthrene, Phenanthren-9-o, 9-Phenanthrenol) is a selective TRPM4 inhibitor with an IC50 in the range of 0.02 μM, without effects on TRPM5.

Sep 01 2021