Bcl-2

Inhibitory Selectivity

Isoform-specific Inhibitors

Bcl-2 Products

All (42) Bcl-2 Inhibitors (25) Bcl-2 Activators (8) Bcl-2 Antagonists (5) Bcl-2 Modulators (4) New Bcl-2 Products

Catalog No.	Information	Product Use Citations	Product Validations
S1002	ABT-737 ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. ABT-737 induces mitochondrial pathway apoptosis and mitophagy. Phase 2.	Cancer Cell, 2022, S1535-6108(22)00312-9 Signal Transduct Target Ther, 2022, 7(1):51 Blood, 2022, blood.2021014304	Cardiomyocytes transduced with or without Ad-Mst1 were treated with ABT-737 (0, 0.1, 1, 10 uM) for 12 hours. Representative immunoblots with antibodies to p62/SQSTM1, LC3 and GAPDH are shown.
S1121	TW-37 TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with K_i of 0.29 μM, 1.11 μM and 0.26 μM in cell-free assays, respectively.	J Cell Mol Med, 2022, 10.1111/jcmm.17210 iScience, 2021, 24(9):103080 Platelets, 2020, 10.1080/09537104.2020.1724276	(a) H23 cells exposed for 0–24 h to TW-37 (10 uM) with and without ZVAD.fmk (50 uM) were monitored for apoptotic morphology using electron microscopy (scale bar, 5 mm). % PS positive cells indicate the percentage of apoptotic cells, characterised by PS externalisation.
S2812	(R)-(-)-Gossypol acetic acid (R)-(-)-Gossypol (AT-101) acetic acid, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with K_i of 0.32 μM, 0.48 μM and 0.18 μM in cell-free assays; does not inhibit BIR3 domain and BID. AT-101 simultaneously triggers apoptosis and a cytoprotective type of autophagy. Phase 2.	Cancer Cell, 2022, S1535-6108(22)00312-9 Eur J Pharm Sci, 2020, 142:105105 Platelets, 2020, 10.1080/09537104.2020.1724276	(B and C) assessment of antimigration capacity in each group by transwell migration assay. Abbreviations: CDDP, cisplatin; DMSO, dimethyl sulfoxide.
S9970^New	APG-2575 (lisaftoclax) APG-2575 (lisaftoclax) is a dual Bcl-2 and Bcl-xl inhibitor with IC50 values of 2 nM and 5.9 nM for Bcl-2 and Bcl-xl, respectively.
S3243^New	Zeaxanthin Zeaxanthin, the carotenoid alcohol participates in the xanthophyll cycle, activates the extrinsic apoptosis pathway which induces apoptosis on uveal melanoma cells with IC50 value 40.8 µM.
S8820	Unesbulin (PTC596) Unesbulin (PTC596) is a second-generation BMI-1 inhibitor that accelerates BMI-1 degradation. PTC596 downregulates MCL-1 and induces p53-independent mitochondrial apoptosis. IC50 values at 72 hours ranged from 68 to 340 nM in mantle cell lymphoma (MCL) cell lines.	Cell Death Dis, 2021, 12(5):495 Int J Mol Sci, 2021, 22(18)10107
S3224	Cinobufagin Cinobufagin (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.
S6895	TCPOBOP TCPOBOP is a constitutive androstane receptor (CAR) agonist. TCPOBOP attenuates Fas-induced murine liver injury by altering Bcl-2 proteins.
S8643	AZD5991 AZD5991 is a macrocyclic MCL-1 inhibitor with sub-nanomolar affinity for MCL-1 (Ki = 0.13 nM). The binding affinity of AZD5991 is about 25-fold lower for mouse Mcl-1 vs. human Mcl-1 but only four-fold lower for rat Mcl-1.	Blood, 2022, blood.2021014011 Nat Commun, 2022, 13(1):1606 Cancer Res, 2022, canres.0218.2021
S7790	A-1210477 A-1210477 is a potent and selective MCL-1 inhibitor with K_i and IC50 of 0.454 nM and 26.2 nM, respectively, >100-fold selectivity over other Bcl-2 family members.	Blood, 2022, blood.2021014304 Cell Death Dis, 2022, 13(5):436 Cell Death Dis, 2021, 12(8):736	U251 glioblastoma (F) or MeWo melanoma (G) cells were treated with selective BH-3 mimetics, GTPP or the combination of both for 24 h (U251) or 48 h (MeWo). Thereafter, cells were stained with annexin V and propidium iodide and analyzed by flow cytometry. Shown are representative flow plots.
S8759	S55746 S55746 (S 055746,BCL201) is a novel, orally active BCL-2 specific inhibitor (Ki = 1.3 nM) with poor affinity for BCL-XL and no significant binding to MCL-1, BFL-1 (BCL2A1/A1). The selectivity of S55746 for BCL-2 versus BCL-XL ranges from ~70 to 400 folds.	Signal Transduct Target Ther, 2022, 7(1):51
S2271	Berberine chloride (NSC 646666) Berberine chloride (NSC 646666, Natural Yellow 18) is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.	J Biomol Struct Dyn, 2022, 1-11 Front Pharmacol, 2021, 12:632201 Molecules, 2021, 26(5)1210
S2448	Gambogic Acid Gambogic Acid (Guttatic Acid, Guttic Acid, Beta-Guttiferrin) activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-X_L, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50 of 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 μM, respectively.	Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-0775
S8383	S63845 S63845 is a new, selective MCL-1 inhibitor with the Kd value of 0.19 nM and has no discernible binding to the other BCL-2 members, BCL-2 or BCL-XL.	Signal Transduct Target Ther, 2022, 7(1):51 Nat Commun, 2022, 13(1):1606 Oncogene, 2022, 10.1038/s41388-022-02200-5
S5967	Berberine chloride hydrate Berberine (Natural Yellow 18) chloride hydrate is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.	Front Pharmacol, 2021, 12:632201
S5600	Flavokawain A Flavokawain A, extracted from kava, is an apoptotic inducers and anticarcinogenic agent. Flavokawain A can down-regulation of antiapoptotic proteins, such as XIAP, survivin, and Bcl-xL, thereby changing the balance between apoptotic and antiapoptotic molecules and then induce cell death in tumor cells.
S8177	BH3I-1 BH3I-1 is a Bcl-X_L-BH3 domain interaction inhibitor with Ki of 2.4 μM (by fluorescence polarization ).It is a selective inhibitor of Bcl-2 family proteins.
S8865	BAI1 BAI1 is a direct allosteric inhibitor of BAX with a dissociation constant (Kd) of 15.0 ± 4 μM.	Cell Rep Methods, 2022, 2(3)100174 Cell Death Dis, 2021, 12(11):1050
S6852	Gossypol Gossypol (BL 193) is an orally-active polyphenol isolated from cotton seeds and roots. Gossypol is a potent inhibitor of 5α-reductase 1 and 3α-hydroxysteroid dehydrogenase with IC50 of 3.33 μM and 0.52 μM in cell-free assay, respectively. Gossypol also inhibits the binding of BH3 peptide to Bcl protein with IC50 of 0.4 μM and 10 μM for Bcl-XL and Bcl-2, respectively. Gossypol induces apoptosis and cell growth inhibition in various cancer cells.	Mol Med Rep, 2021, 23(1)40 J Biol Chem, 2015, 290(34):20841-55
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.
S8758	VU661013 VU661013 is a novel, potent, selective MCL1 inhibitor with Ki of 97 ± 30 pM of human MCL-1 in a TR-FRET assay. However, VU661013 does not significantly inhibit BCL-xL or BCL-2 with Ki > 40 μM or = 0.73 μM. VU661013 de-stabilizes BIM/MCL-1 association, leads to apoptosis in AML.
S7800	A-1155463 A-1155463, a highly potent and selective BCL-XL inhibitor, shows picomolar binding affinity to BCL-XL, and >1000-fold weaker binding to BCL-2 and related proteins BCL-W(Ki=19 nM) and MCL-1(Ki>440 nM).	J Immunother Cancer, 2022, 10(3)e004348 ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138 Pharmacol Res, 2022, 177:106095	Tumor growth rate (TGR) of tumors orthotopically implanted in rats on day 3, 7 and 10 compared to day 0. Rats were treated with doxorubicin, A-1155463 or a combination. Treatment with A-1155463 resulted in a significant decrease in TGR compared to control mice.
S7801	A-1331852 A-1331852 is a potent and selectiveBCL-XL inhibitor with Ki value less than 0.01 nM for BCL-XL and 6 nM, 4 nM, 142 nM for Bcl-2, Bcl-W, MCL-1 respectively. It may be useful in the treatment of cancer, immune and autoimmune diseases.	Nat Commun, 2022, 13(1):1199 Cell Death Dis, 2022, 13(5):436 ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138	Cells were treated with 0.5 μM A-1331852 and 1.5 nM VCR (RD), 0.5 nM VCR (RH30) for 72 h. Apoptosis was determined by analysis of DNA fragmentation of PI-stained nuclei using flow cytometry. Mean and SD of three independent experiments performed in triplicate are shown; **P < 0.01.
S7531	UMI-77 UMI-77 is a selective Mcl-1 inhibitor with Ki of 490 nM, showing selectivity over other members of Bcl-2 family.	Blood, 2022, blood.2021014304 Haematologica, 2021, 10.3324/haematol.2021.278369 Cell Chem Biol, 2021, S2451-9456(21)00213-0	U87 and A172 cells were treated with UMI-77 (8 μM) for 24h and further treated with TRAIL (30 ng/ml) for indicated period of time. Levels of apoptosis-associated proteins were analyzed by Western blot. GAPDH was used as a loading control.
S8836	S64315 (MIK665) S64315 (MIK665) is an inhibitor of induced myeloid leukemia cell differentiation protein Mcl-1 with Ki value of 1.2 nM and has potential pro-apoptotic and antineoplastic activities.	Cell Death Dis, 2020, 8;11(6):443 Blood Adv, 2020, 4(5):819-829 Cancers (Basel), 2020, 12(8):E2182
S7105	BAM7 BAM 7 is a direct and selective activator of proapoptotic Bax with EC50 of 3.3 μM.	Nat Chem Biol, 2019, 15(4):322-330 Cell Death Discov, 2018, 4:107
E2354^New	Valepotriate Valepotriate, an unstable iridoid isolated from Valeriana jatamansi Jones, has anti-epileptic by significantly increasing the expression of GABA_A, glutamic acid decarboxylase 65, and Bcl-2 and reduce the expression of caspase-3.
S8650	BTSA1 BTSA1 is a pharmacologically optimized BAX activator that binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis. It effectively promotes apoptosis in leukemia cell lines and patient samples while sparing healthy cells.	Cell Death Dis, 2021, 12(11):1050 Life Sci, 2021, S0024-3205(21)01048-1
S3238	Resibufogenin Resibufogenin (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.	Phytomedicine, 2022, 102:154182
S3275	Senkyunolide I Senkyunolide I (SEI, SENI) is an orally active compound isolated from Ligusticum chuanxiong with analgesic, anti-migraine, neuroprotective, anti-oxidation and anti-apoptosis activities. Senkyunolide I (SEI, SENI) up-regulates the phosphorylation of Erk1/2 and induces Nrf2 nuclear translocation with enhanced HO-1 and NQO1 expressions. Senkyunolide I (SEI, SENI) promotes the ratio of Bcl-2/Bax and inhibits the expressions of cleaved caspase 3 and caspase 9.	Cell Commun Signal, 2021, 19(1):115
S7747	Ro-3306 RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with K_i of 20 nM, >15-fold selectivity against a diverse panel of human kinases. RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis.	Blood, 2022, blood.2021014304 DNA Repair (Amst), 2022, 116:103354 Mol Cancer Res, 2022, molcanres.0612.2021	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.
S9276	Alisol B Alisol B, a triterpene from Alismatis rhizoma, induces Bax up-regulation and nuclear translocation, the activation of initiator caspase-8 and caspase-9, and executor caspase-3, suggesting the involvement of both extrinsic and intrinsic apoptosis pathways.
S6990	Phytohemagglutinin Phytohemagglutinin (PHA, Phaseolus vulgaris agglutinin) is expressed in Pichia pastoris using native signal peptides, or the Saccharomyces alpha-factor preprosequence, to direct proteins into the secretory pathway. Phytohemagglutinin induces apoptosis in human HEp-2 carcinoma cells via increasing proapoptotic protein Bax and activating caspases-3.
S7849	BDA-366 BDA-366 is a small-molecule Bcl2-BH4 domain antagonist and binds BH4 with high affinity and selectivity. It directly binds to Bcl2 with high binding affinity (Ki =3.3 ± 0.73 nM).
E0124^New	Chelerythrine Chelerythrine (Toddaline, Broussonpapyrine) is a potent, selective antagonist of PKC with an IC50 of 0.66 μM. Chelerythrine also inhibits the BclXL-Bak BH3 peptide binding with an IC50 of 1.5 μM. Chelerythrine shows antitumor, antidiabetic and anti-inflammatory activity.	Nutr Neurosci, 2022, 1-19
S7100	WEHI-539 HCl WEHI-539 HCl (WEHI-539 hydrochloride) has high affinity (IC50=1.1 nM) and selectivity for BCL-XL and potently kills cells by selectively antagonizing its prosurvival activity. It has more than a 400-fold higher affinity for BCL-XL versus other prosurvival BCL-2 family members.	Cell Death Differ, 2021, 10.1038/s41418-021-00816-w Commun Biol, 2021, 4(1):20 Mol Pharmacol, 2019, 96(4):419-429
S7126	Marinopyrrole A (Maritoclax) Marinopyrrole A (Maritoclax) is a selective Mcl-1 antagonist. It binds to Mcl-1, but not Bcl-XL, and targets Mcl-1 for proteasomal degradation. Maritoclax disrupts the interaction between Bim and Mcl-1 with an IC50 of 10.1 μM.	Cell Signal, 2022, S0898-6568(22)00041-9 Leukemia, 2019, 33(2):319-332 Molecules, 2018, 23(11)E3030
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.	Emerg Microbes Infect, 2022, 1-29 Front Cell Dev Biol, 2021, 9:765973
E2028^New	Humanin (human) Humanin (human) (1-24-Protein humanin (human)), a small mitochondrial-derived cytoprotective polypeptide encoded by mtDNA, exhibits protective effects in several cell types against cellular stress conditions and apoptosis through regulating various signaling mechanisms, such as JAK/STAT pathway and interaction of BCL-2 family of protein.
S3245	Nodakenetin Nodakenetin (NANI), a plant-derived coumarin isolated from Angelica decursiva, inhibits α-glucosidase, PTP1B, rat lens aldose reductase (RLAR), AChE, BChE, and β-site amyloid precursor protein cleaving enzyme 1 (BACE1). Nodakenetin alters the protein expression of Bax and Bcl-2, and prompts mitochondrial apoptosis. Nodakenetin exhibits anti-tumor activity.
S3267	Kaempferol-3-O-rutinoside Kaempferol-3-O-rutinoside (Nicotiflorin, Nikotoflorin, Kaempferol 3-O-β-rutinoside), a flavonoid extracted from Carthamus tinctorius, alters the shape and structure of injured neurons, decreases the number of apoptotic cells, down-regulates expression of p-JAK2, p-STAT3, caspase-3, and Bax and decreases Bax immunoredactivity, and increases Bcl-2 protein expression and immunoreactivity.
S0563	10-Deacetyl-7-xylosyl paclitaxel 10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol, 7-xylosyl-10-deacetylpaclitaxel), a derivative of paclitaxel and naturally occurring xyloside isolated from Taxus chinensis, causes significant mitotic arrest in PC-3 cells followed by up-regulating expression of pro-apoptotic Bax and Bad protein, as well as down-regulating expression of anti-apoptotic Bcl-2 and Bcl-XL , which leads to a disturbance of the mitochondrial membrane permeability and to the activation of caspase-9.

Catalog No.	Information	Product Use Citations	Product Validations
S1002	ABT-737 ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. ABT-737 induces mitochondrial pathway apoptosis and mitophagy. Phase 2.	Cancer Cell, 2022, S1535-6108(22)00312-9 Signal Transduct Target Ther, 2022, 7(1):51 Blood, 2022, blood.2021014304	Cardiomyocytes transduced with or without Ad-Mst1 were treated with ABT-737 (0, 0.1, 1, 10 uM) for 12 hours. Representative immunoblots with antibodies to p62/SQSTM1, LC3 and GAPDH are shown.
S1121	TW-37 TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with K_i of 0.29 μM, 1.11 μM and 0.26 μM in cell-free assays, respectively.	J Cell Mol Med, 2022, 10.1111/jcmm.17210 iScience, 2021, 24(9):103080 Platelets, 2020, 10.1080/09537104.2020.1724276	(a) H23 cells exposed for 0–24 h to TW-37 (10 uM) with and without ZVAD.fmk (50 uM) were monitored for apoptotic morphology using electron microscopy (scale bar, 5 mm). % PS positive cells indicate the percentage of apoptotic cells, characterised by PS externalisation.
S2812	(R)-(-)-Gossypol acetic acid (R)-(-)-Gossypol (AT-101) acetic acid, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with K_i of 0.32 μM, 0.48 μM and 0.18 μM in cell-free assays; does not inhibit BIR3 domain and BID. AT-101 simultaneously triggers apoptosis and a cytoprotective type of autophagy. Phase 2.	Cancer Cell, 2022, S1535-6108(22)00312-9 Eur J Pharm Sci, 2020, 142:105105 Platelets, 2020, 10.1080/09537104.2020.1724276	(B and C) assessment of antimigration capacity in each group by transwell migration assay. Abbreviations: CDDP, cisplatin; DMSO, dimethyl sulfoxide.
S9970^New	APG-2575 (lisaftoclax) APG-2575 (lisaftoclax) is a dual Bcl-2 and Bcl-xl inhibitor with IC50 values of 2 nM and 5.9 nM for Bcl-2 and Bcl-xl, respectively.
S3243^New	Zeaxanthin Zeaxanthin, the carotenoid alcohol participates in the xanthophyll cycle, activates the extrinsic apoptosis pathway which induces apoptosis on uveal melanoma cells with IC50 value 40.8 µM.
S8820	Unesbulin (PTC596) Unesbulin (PTC596) is a second-generation BMI-1 inhibitor that accelerates BMI-1 degradation. PTC596 downregulates MCL-1 and induces p53-independent mitochondrial apoptosis. IC50 values at 72 hours ranged from 68 to 340 nM in mantle cell lymphoma (MCL) cell lines.	Cell Death Dis, 2021, 12(5):495 Int J Mol Sci, 2021, 22(18)10107
S3224	Cinobufagin Cinobufagin (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.
S6895	TCPOBOP TCPOBOP is a constitutive androstane receptor (CAR) agonist. TCPOBOP attenuates Fas-induced murine liver injury by altering Bcl-2 proteins.
S8643	AZD5991 AZD5991 is a macrocyclic MCL-1 inhibitor with sub-nanomolar affinity for MCL-1 (Ki = 0.13 nM). The binding affinity of AZD5991 is about 25-fold lower for mouse Mcl-1 vs. human Mcl-1 but only four-fold lower for rat Mcl-1.	Blood, 2022, blood.2021014011 Nat Commun, 2022, 13(1):1606 Cancer Res, 2022, canres.0218.2021
S7790	A-1210477 A-1210477 is a potent and selective MCL-1 inhibitor with K_i and IC50 of 0.454 nM and 26.2 nM, respectively, >100-fold selectivity over other Bcl-2 family members.	Blood, 2022, blood.2021014304 Cell Death Dis, 2022, 13(5):436 Cell Death Dis, 2021, 12(8):736	U251 glioblastoma (F) or MeWo melanoma (G) cells were treated with selective BH-3 mimetics, GTPP or the combination of both for 24 h (U251) or 48 h (MeWo). Thereafter, cells were stained with annexin V and propidium iodide and analyzed by flow cytometry. Shown are representative flow plots.
S8759	S55746 S55746 (S 055746,BCL201) is a novel, orally active BCL-2 specific inhibitor (Ki = 1.3 nM) with poor affinity for BCL-XL and no significant binding to MCL-1, BFL-1 (BCL2A1/A1). The selectivity of S55746 for BCL-2 versus BCL-XL ranges from ~70 to 400 folds.	Signal Transduct Target Ther, 2022, 7(1):51
S2271	Berberine chloride (NSC 646666) Berberine chloride (NSC 646666, Natural Yellow 18) is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.	J Biomol Struct Dyn, 2022, 1-11 Front Pharmacol, 2021, 12:632201 Molecules, 2021, 26(5)1210
S2448	Gambogic Acid Gambogic Acid (Guttatic Acid, Guttic Acid, Beta-Guttiferrin) activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-X_L, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50 of 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 μM, respectively.	Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-0775
S8383	S63845 S63845 is a new, selective MCL-1 inhibitor with the Kd value of 0.19 nM and has no discernible binding to the other BCL-2 members, BCL-2 or BCL-XL.	Signal Transduct Target Ther, 2022, 7(1):51 Nat Commun, 2022, 13(1):1606 Oncogene, 2022, 10.1038/s41388-022-02200-5
S5967	Berberine chloride hydrate Berberine (Natural Yellow 18) chloride hydrate is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.	Front Pharmacol, 2021, 12:632201
S5600	Flavokawain A Flavokawain A, extracted from kava, is an apoptotic inducers and anticarcinogenic agent. Flavokawain A can down-regulation of antiapoptotic proteins, such as XIAP, survivin, and Bcl-xL, thereby changing the balance between apoptotic and antiapoptotic molecules and then induce cell death in tumor cells.
S8177	BH3I-1 BH3I-1 is a Bcl-X_L-BH3 domain interaction inhibitor with Ki of 2.4 μM (by fluorescence polarization ).It is a selective inhibitor of Bcl-2 family proteins.
S8865	BAI1 BAI1 is a direct allosteric inhibitor of BAX with a dissociation constant (Kd) of 15.0 ± 4 μM.	Cell Rep Methods, 2022, 2(3)100174 Cell Death Dis, 2021, 12(11):1050
S6852	Gossypol Gossypol (BL 193) is an orally-active polyphenol isolated from cotton seeds and roots. Gossypol is a potent inhibitor of 5α-reductase 1 and 3α-hydroxysteroid dehydrogenase with IC50 of 3.33 μM and 0.52 μM in cell-free assay, respectively. Gossypol also inhibits the binding of BH3 peptide to Bcl protein with IC50 of 0.4 μM and 10 μM for Bcl-XL and Bcl-2, respectively. Gossypol induces apoptosis and cell growth inhibition in various cancer cells.	Mol Med Rep, 2021, 23(1)40 J Biol Chem, 2015, 290(34):20841-55
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.
S8758	VU661013 VU661013 is a novel, potent, selective MCL1 inhibitor with Ki of 97 ± 30 pM of human MCL-1 in a TR-FRET assay. However, VU661013 does not significantly inhibit BCL-xL or BCL-2 with Ki > 40 μM or = 0.73 μM. VU661013 de-stabilizes BIM/MCL-1 association, leads to apoptosis in AML.
S7800	A-1155463 A-1155463, a highly potent and selective BCL-XL inhibitor, shows picomolar binding affinity to BCL-XL, and >1000-fold weaker binding to BCL-2 and related proteins BCL-W(Ki=19 nM) and MCL-1(Ki>440 nM).	J Immunother Cancer, 2022, 10(3)e004348 ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138 Pharmacol Res, 2022, 177:106095	Tumor growth rate (TGR) of tumors orthotopically implanted in rats on day 3, 7 and 10 compared to day 0. Rats were treated with doxorubicin, A-1155463 or a combination. Treatment with A-1155463 resulted in a significant decrease in TGR compared to control mice.
S7801	A-1331852 A-1331852 is a potent and selectiveBCL-XL inhibitor with Ki value less than 0.01 nM for BCL-XL and 6 nM, 4 nM, 142 nM for Bcl-2, Bcl-W, MCL-1 respectively. It may be useful in the treatment of cancer, immune and autoimmune diseases.	Nat Commun, 2022, 13(1):1199 Cell Death Dis, 2022, 13(5):436 ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138	Cells were treated with 0.5 μM A-1331852 and 1.5 nM VCR (RD), 0.5 nM VCR (RH30) for 72 h. Apoptosis was determined by analysis of DNA fragmentation of PI-stained nuclei using flow cytometry. Mean and SD of three independent experiments performed in triplicate are shown; **P < 0.01.
S7531	UMI-77 UMI-77 is a selective Mcl-1 inhibitor with Ki of 490 nM, showing selectivity over other members of Bcl-2 family.	Blood, 2022, blood.2021014304 Haematologica, 2021, 10.3324/haematol.2021.278369 Cell Chem Biol, 2021, S2451-9456(21)00213-0	U87 and A172 cells were treated with UMI-77 (8 μM) for 24h and further treated with TRAIL (30 ng/ml) for indicated period of time. Levels of apoptosis-associated proteins were analyzed by Western blot. GAPDH was used as a loading control.
S8836	S64315 (MIK665) S64315 (MIK665) is an inhibitor of induced myeloid leukemia cell differentiation protein Mcl-1 with Ki value of 1.2 nM and has potential pro-apoptotic and antineoplastic activities.	Cell Death Dis, 2020, 8;11(6):443 Blood Adv, 2020, 4(5):819-829 Cancers (Basel), 2020, 12(8):E2182

Catalog No.	Information	Product Use Citations	Product Validations
S7105	BAM7 BAM 7 is a direct and selective activator of proapoptotic Bax with EC50 of 3.3 μM.	Nat Chem Biol, 2019, 15(4):322-330 Cell Death Discov, 2018, 4:107
E2354^New	Valepotriate Valepotriate, an unstable iridoid isolated from Valeriana jatamansi Jones, has anti-epileptic by significantly increasing the expression of GABA_A, glutamic acid decarboxylase 65, and Bcl-2 and reduce the expression of caspase-3.
S8650	BTSA1 BTSA1 is a pharmacologically optimized BAX activator that binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis. It effectively promotes apoptosis in leukemia cell lines and patient samples while sparing healthy cells.	Cell Death Dis, 2021, 12(11):1050 Life Sci, 2021, S0024-3205(21)01048-1
S3238	Resibufogenin Resibufogenin (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.	Phytomedicine, 2022, 102:154182
S3275	Senkyunolide I Senkyunolide I (SEI, SENI) is an orally active compound isolated from Ligusticum chuanxiong with analgesic, anti-migraine, neuroprotective, anti-oxidation and anti-apoptosis activities. Senkyunolide I (SEI, SENI) up-regulates the phosphorylation of Erk1/2 and induces Nrf2 nuclear translocation with enhanced HO-1 and NQO1 expressions. Senkyunolide I (SEI, SENI) promotes the ratio of Bcl-2/Bax and inhibits the expressions of cleaved caspase 3 and caspase 9.	Cell Commun Signal, 2021, 19(1):115
S7747	Ro-3306 RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with K_i of 20 nM, >15-fold selectivity against a diverse panel of human kinases. RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis.	Blood, 2022, blood.2021014304 DNA Repair (Amst), 2022, 116:103354 Mol Cancer Res, 2022, molcanres.0612.2021	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.
S9276	Alisol B Alisol B, a triterpene from Alismatis rhizoma, induces Bax up-regulation and nuclear translocation, the activation of initiator caspase-8 and caspase-9, and executor caspase-3, suggesting the involvement of both extrinsic and intrinsic apoptosis pathways.
S6990	Phytohemagglutinin Phytohemagglutinin (PHA, Phaseolus vulgaris agglutinin) is expressed in Pichia pastoris using native signal peptides, or the Saccharomyces alpha-factor preprosequence, to direct proteins into the secretory pathway. Phytohemagglutinin induces apoptosis in human HEp-2 carcinoma cells via increasing proapoptotic protein Bax and activating caspases-3.

Catalog No.	Information	Product Use Citations
S7849	BDA-366 BDA-366 is a small-molecule Bcl2-BH4 domain antagonist and binds BH4 with high affinity and selectivity. It directly binds to Bcl2 with high binding affinity (Ki =3.3 ± 0.73 nM).
E0124^New	Chelerythrine Chelerythrine (Toddaline, Broussonpapyrine) is a potent, selective antagonist of PKC with an IC50 of 0.66 μM. Chelerythrine also inhibits the BclXL-Bak BH3 peptide binding with an IC50 of 1.5 μM. Chelerythrine shows antitumor, antidiabetic and anti-inflammatory activity.	Nutr Neurosci, 2022, 1-19
S7100	WEHI-539 HCl WEHI-539 HCl (WEHI-539 hydrochloride) has high affinity (IC50=1.1 nM) and selectivity for BCL-XL and potently kills cells by selectively antagonizing its prosurvival activity. It has more than a 400-fold higher affinity for BCL-XL versus other prosurvival BCL-2 family members.	Cell Death Differ, 2021, 10.1038/s41418-021-00816-w Commun Biol, 2021, 4(1):20 Mol Pharmacol, 2019, 96(4):419-429
S7126	Marinopyrrole A (Maritoclax) Marinopyrrole A (Maritoclax) is a selective Mcl-1 antagonist. It binds to Mcl-1, but not Bcl-XL, and targets Mcl-1 for proteasomal degradation. Maritoclax disrupts the interaction between Bim and Mcl-1 with an IC50 of 10.1 μM.	Cell Signal, 2022, S0898-6568(22)00041-9 Leukemia, 2019, 33(2):319-332 Molecules, 2018, 23(11)E3030
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.	Emerg Microbes Infect, 2022, 1-29 Front Cell Dev Biol, 2021, 9:765973

Catalog No.	Information	Product Use Citations	Product Validations
E2028^New	Humanin (human) Humanin (human) (1-24-Protein humanin (human)), a small mitochondrial-derived cytoprotective polypeptide encoded by mtDNA, exhibits protective effects in several cell types against cellular stress conditions and apoptosis through regulating various signaling mechanisms, such as JAK/STAT pathway and interaction of BCL-2 family of protein.
S3245	Nodakenetin Nodakenetin (NANI), a plant-derived coumarin isolated from Angelica decursiva, inhibits α-glucosidase, PTP1B, rat lens aldose reductase (RLAR), AChE, BChE, and β-site amyloid precursor protein cleaving enzyme 1 (BACE1). Nodakenetin alters the protein expression of Bax and Bcl-2, and prompts mitochondrial apoptosis. Nodakenetin exhibits anti-tumor activity.
S3267	Kaempferol-3-O-rutinoside Kaempferol-3-O-rutinoside (Nicotiflorin, Nikotoflorin, Kaempferol 3-O-β-rutinoside), a flavonoid extracted from Carthamus tinctorius, alters the shape and structure of injured neurons, decreases the number of apoptotic cells, down-regulates expression of p-JAK2, p-STAT3, caspase-3, and Bax and decreases Bax immunoredactivity, and increases Bcl-2 protein expression and immunoreactivity.
S0563	10-Deacetyl-7-xylosyl paclitaxel 10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol, 7-xylosyl-10-deacetylpaclitaxel), a derivative of paclitaxel and naturally occurring xyloside isolated from Taxus chinensis, causes significant mitotic arrest in PC-3 cells followed by up-regulating expression of pro-apoptotic Bax and Bad protein, as well as down-regulating expression of anti-apoptotic Bcl-2 and Bcl-XL , which leads to a disturbance of the mitochondrial membrane permeability and to the activation of caspase-9.

Choose Your Country or Region

By Signaling Pathways

By product type

Bcl-2

Inhibitory Selectivity

Isoform-specific Inhibitors

Bcl-2 Products