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Bcl-2 Family

Bcl-2 Family

Inhibitory Selectivity

Catalog No.	Inhibitor Name	Bcl-2	Bcl-B	Bcl-w	Bcl-xL	Mcl-1	A1	Bax	Other
A10255	ABT-737	****	*	***	***
A10022	Navitoclax (ABT-263)	****		****	****	**	**
A10665	Obatoclax Mesylate	***
A10955	TW-37	***			*	***
A12500	Venetoclax	****		***	****
A15004	AT101	**			**	***
A11448	HA14-1	*
A12823	Sabutoclax	**			**	***		**
A15545	A-1210477					****
A14222	UMI-77					**
A11988	Gambogic Acid	*	*	****	*	*		*	Caspase
A12743	BM-1074	****			****
A13327	WEHI-539 hydrochloride				****
A15821	BDA-366	***
A16061	BH3I-1				*				p53
A16112	A-1155463				****
A16190	A-1331852				****
A16314	Apogossypolone (ApoG2)

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Bcl-2 Family Products Bcl-2 Family New Products Compare Solubility

Catalog No.	Product Name	Application	Product Information
A10022 SALE	ABT-263 (Navitoclax)	Bcl-2 inhibitor	ABT-263 also called Navitoclax is a potent and orally bioavailable Bcl-2 family inhibitor (Ki's of <1 nmol/L for Bcl-2, Bcl-xL, and Bcl-w).ABT-263 maintains a high affinity for Bcl-xL, Bcl-2, and Bcl-w, (Ki ≤1 nmol/L), but binds more weakly to Mcl-1 and A1.^[1] Product Citations (10) Momeny M, .et al. The ERBB receptor inhibitor dacomitinib suppresses proliferation and invasion of pancreatic ductal adenocarcinoma cells, Cell Oncol (Dordr), 2019, Apr 25 PMID: 31025257 Anderson R, .et al. Length-independent telomere damage drives postmitotic cardiomyocyte senescence, EMBO J, 2019, Feb 8. pii: e100492 PMID: 30737259 Shinya Ishida, .et al. Mechanisms for mTORC1 activation and synergistic induction of apoptosis by ruxolitinib and BH3 mimetics or autophagy inhibitors in JAK2-V617F-expressing leukemic cells including newly established PVTL-2, Oncotarget, 2018, Jun 1; 9(42): 26834-26851 PMID: 29928488 Rhys Anderson, .et al. Length-independent telomere damage drives cardiomyocyte senescence, bioRxiv, 2018, 2018 Ryuta Mikawa, .et al. Elimination of p19ARF-expressing cells protects against pulmonary emphysema in mice, Aging Cell, 2018, Oct; 17(5): e12827 PMID: 30058137 Joo Sang Lee, .et al. Harnessing synthetic lethality to predict the response to cancer treatment, Nat Commun, 2018, 9: 2546 PMID: 29959327 Toshiyuki Sumi, .et al. Survivin knockdown induces senescence in TTF-1-expressing, KRAS-mutant lung adenocarcinomas, Int J Oncol, 2018, Jul; 53(1): 33-46 PMID: 29658609 Wei TW, .et al. Aurora A and NF-κB Survival Pathway Drive Chemoresistance in Acute Myeloid Leukemia via the TRAF-Interacting Protein TIFA, Cancer Res, 2017, Jan 15;77(2):494-508 PMID: 28069801 Yusuke Takagi, .et al. SPIB is a novel prognostic factor in diffuse large B-cell lymphoma that mediates apoptosis via the PI3K-AKT pathway, Cancer Sci, 2016, Sep; 107(9): 1270-1280 PMID: 27348272 Matsumoto M, .et al. Cisplatin-induced apoptosis in non-small-cell lung cancer cells is dependent on Bax- and Bak-induction pathway and synergistically activated by BH3-mimetic ABT-263 in p53 wild-type and mutant cells, Biochem Biophys Res Commun, 2016, Apr 29;473(2):490-6 PMID: 26996126
A10255 SALE	ABT-737	Bcl-2 Inhibitor	ABT-737 is a pan-Bcl-2 inhibitor. IC50 values ranged from 192 nM (the pre-B cell line Hal-01) to <10 μM (Nalm-6, K562 and HL-60). Product Citations (6) Meikle V, .et al. A protein complex from human milk enhances the activity of antibiotics and drugs against Mycobacterium tuberculosis, Antimicrob Agents Chemother, 2018, Nov 12. pii: AAC.01846-18 PMID: 30420480 Chauhan D, .et al. BAX/BAK-Induced Apoptosis Results in Caspase-8-Dependent IL-1β Maturation in Macrophages, Cell Rep, 2018, Nov 27;25(9):2354-2368.e5 PMID: 30485805 Jose Mario Gonzalez-Meljem, .et al. Stem cell senescence drives age-attenuated induction of pituitary tumours in mouse models of paediatric craniopharyngioma, Nat Commun, 2017, 8: 1819 PMID: 29180744 Zhang C, .et al. Sorafenib targets the mitochondrial electron transport chain complexes and ATP synthase to activate the PINK1-Parkin pathway and modulate cellular drug response, J Biol Chem, 2017, Sep 8;292(36):15105-15120 PMID: 28673964 Eun Young Kim, .et al. ABT-737 Synergizes with Cisplatin Bypassing Aberration of Apoptotic Pathway in Non-small Cell Lung Cancer, Neoplasia, 2017, Apr; 19(4): 354-363 PMID: 28319809 Masayoshi Toge, .et al. Critical contribution of MCL-1 in EMT-associated chemo-resistance in A549 non-small cell lung cancer., Int J Oncol., 2015, Apr;46(4):1844-8 PMID: 25647738
A13005	WEHI539	Bcl-XL inhibitor	WEHI539 is a selective inhibitor of Bcl-XL with IC50 of 1.1 nM.
A12500 SALE	ABT-199 (Venetoclax)	Bcl-2 inhibitor	ABT-199 is a so-called BH3-mimetic drug, which is designed to block the function of the protein Bcl 2. Product Citations (3) Chauhan D, .et al. BAX/BAK-Induced Apoptosis Results in Caspase-8-Dependent IL-1β Maturation in Macrophages, Cell Rep, 2018, Nov 27;25(9):2354-2368.e5 PMID: 30485805 Martin Grundy, .et al. Predicting effective pro-apoptotic anti-leukaemic drug combinations using co-operative dynamic BH3 profiling, PLoS One, 2018, 13(1): e0190682 PMID: 29298347 Joanne Dai, .et al. Intracellular BH3 profiling reveals shifts in anti-apoptotic dependency in B-cell maturation and activation, J Immunol, 2018, 200 (5) 1727-1736 PMID: 29358277
A10665 SALE	Obatoclax mesylate (GX15-070)	Bcl-2 Inhibitor	Bcl-2 homology domain-3 (BH3) mimetic,antagonize all antiapoptotic Bcl-2 family proteins (average IC50, 3 umol/L), including Mcl-1 (IC50, 2.9 umol/L) and Bfl-1 (IC50, 5 umol/L). Product Citations (2) Chi-Hung R. Or, .et al. Obatoclax, a Pan-BCL-2 Inhibitor, Targets Cyclin D1 for Degradation to Induce Antiproliferation in Human Colorectal Carcinoma Cells, Int J Mol Sci, 2016, Jan; 18(1): 44 PMID: 28035994 P Geserick, .et al. The ratio of Mcl-1 and Noxa determines ABT737 resistance in squamous cell carcinoma of the skin, Cell Death Dis., 2014, 5(9): e1412 PMID: 25210795
A16315	MIM1	Mcl-1 inhibitor	MIM1 is a selective small molecule inhibitor of Mcl-1(IC50= 4.8 μM) that overcomes Mcl-1-dependent leukemia cell survival. Product Citations (1) Yubao Wang ,etc. Mitotic MELK-eIF4B signaling controls protein synthesis and tumor cell survival. Proc Natl Acad Sci USA. 2016 Aug 30; 113(35): 9810–9815.
A11448 SALE	HA14-1	Bcl-2 inhibitor	HA14-1 interacts with Bcl-2 and inhibits the antiapoptotic effect of Bcl-2.
A14222 SALE	UMI-77	Mcl-1 inhibitor	UMI-77 is a selective Mcl-1 inhibitor with Ki of 490 nM, showing selectivity over other members of Bcl-2 family.
A15004	AT-101	Bcl-2 Inhibitor	AT101, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32μM, 0.48μM and 0.18μM.
A12823	Sabutoclax	Bcl-2 inhibitor	Sabutoclax(BI-97C1) is a pan-Bcl-2 inhibitor, including Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively. Product Citations (1) Christopher D. Graham, .et al. BH3 mimetics suppress CXCL12 expression in human malignant peripheral nerve sheath tumor cells, Oncotarget, 2017, Jan 31; 8(5): 8670-8678 PMID: 28055968
A13578	AT101 acetic acid	pan Bcl-2 inhibitor	AT101, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32 μM, 0.48 μM and 0.18 μM; does not inhibit BIR3 domain and BID
A16112	A-1155463	BCL-XL inhibitor	A-1155463 is a highly potent and selective BCL-XL inhibitor, A-1155463 shows picomolar binding affinity to BCL-XL (Ki<0.01 nM), and >1000-fold weaker binding to BCL-2 (Ki = 80 nM) and related proteins BCL-W (Ki = 19 nM) and MCL-1 (Ki > 440 nM) Product Citations (1) Chauhan D, .et al. BAX/BAK-Induced Apoptosis Results in Caspase-8-Dependent IL-1β Maturation in Macrophages, Cell Rep, 2018, Nov 27;25(9):2354-2368.e5 PMID: 30485805
A16190	A-1331852	BCL-XL inhibitor	A-1331852 is a potent and selective BCL-XL inhibitor. BCL-XL is the major antiapoptotic survival protein and may be a novel therapeutic target in CML.
A10955	TW-37	Bcl-2 inhibitor	TW-37, a small-molecule inhibitor of Bcl-2, inhibits cell growth and induces apoptosis in pancreatic cancer mediated through a novel pathway involving inactivation of Notch-1 and Jagged-1.
A16316	(+)-Apogossypol	Bcl-2 family inhibitor	(+)-Apogossypol is a potent inhibitor of Bcl-2 family proteins; competing with the BH3 peptide-binding sites on Bcl-2, Bcl-XL, Mcl-1, Bcl-W, and Bcl-B, but not Bfl-1, with IC50s of 0.5 to 2 μM.
A12743	BM-1074	Bcl-2/Bcl-xL inhibitor	BM-1074 is a potent and efficacious Bcl-2/Bcl-xL inhibitor with Ki of <1 nM.
A16323	(S)-Gossypol acetic acid	Bcl-2 inhibitor	(S)-Gossypol acetic acid is a inhibitor of Bcl-2, potently induce cell death in Jurkat cells overexpressing Bcl-2 (IC50, 18.1μM) or Bcl-xL (IC50, 22.9μM).
A14795	Acetate gossypol	Bcl-2 Inhibitor	Acetate gossypol, a polyphenolic compound isolated from cottonseeds, inhibits Bcl-2 by acting as a BH3 mimetic.
A16314	Apogossypolone (ApoG2)	Bcl-2 inhibitor	Apogossypolone is a nonpeptidic small-molecule inhibitor of Bcl-2 with
A16061 SALE	BH3I-1	Bcl-XL antagonist	BH3I-1 is a cell permeable BH3 mimetic that binds to Bcl-xL
A15821	BDA-366	Bcl-2 antagonist	BDA-366 selectively inhibits BCL2, converting it to a cell death inducer.
A15545	A-1210477	MCL-1 inhibitor	A-1210477 is a potent and selective MCL-1 inhibitor. A-1210477 induces the hallmarks of intrinsic apoptosis and demonstrates single agent killing of multiple myeloma and non-small cell lung cancer cell lines.
A13327	WEHI-539 hydrochloride	Bcl-xL inhibitor	WEHI-539 hydrochloride is a small-molecule inhibitor of BCL-xL with IC50 value of 1.1 nM.
A12907 SALE	BAM 7	Bax activator	BAM 7 binds the BAX trigger site with an EC50 ~ 3.3 μM as measured in a competitive FP assay using FITC-BIM SAHB and BAX.
A13580	Bcl-2 Inhibitor	Bcl-2 Inhibitor	Bcl-2 Inhibitor contains a mixture of two tautomers. A potent, cell-permeable, Bcl-2 inhibitor competes with Bak BH3 peptide for binding to Bcl-2 and Bcl-XL in vitro (IC50 =10 uM and 7 uM, respectively). Product Citations (1) Toshiyuki Sumi, .et al. Survivin knockdown induces senescence in TTF-1-expressing, KRAS-mutant lung adenocarcinomas, Int J Oncol, 2018, Jul; 53(1): 33-46 PMID: 29658609
A16380	Pyridoclax	Mcl-1 inhibitor	Pyridoclax is a potent Mcl-1 inhibitor with Kd value of 25 nM.
A16192	CID5721353	BCL6 inhibitor	CID5721353 is a B-Cell Lymphoma 6 Inhibitor (BCL6 inhibitor).
A15340	Muristerone A	EcR agonist	Muristerone A is a phytoecdysteroid analog of ecdysone which induces genes in mammalian cells and causes apoptosis in cells transfected with wild-type Bax.
A15338	Bax inhibitor peptide, negative control	Bax inhibitor	Bax inhibitor peptide, negative control, negative control peptide for the Bax inhibitor peptides V5 and P5 , which inhibit Bax translocation to mitochondria and Bax-mediated apoptosis in vitro.
A15336	Bax inhibitor peptide P5	Bax inhibitor	Bax inhibitor peptide P5, cell-permeable synthetic peptide inhibitor of Bax translocation to mitochondria; designed from Ku70, a protein that is suggested to suppress the mitochondrial translocation of Bax. Inhibits Bax-mediated apoptosis in vitro.
A15335	Bax channel blocker	Bax channel blocker	Bax channel blocker is a potent inhibitor of Bax-mediated mitochondrial cytochrome C release (IC50 = 0.52 μM).
A11988 SALE	Gambogic acid	Bcl-2 inhibitor	Gambogic acid is a natural product isolated from the Garcinia hanburyi tree. Gambogic Acid activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-XL, 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.
A15337 SALE	Bax inhibitor peptide V5	Bax inhibitor	Bax inhibitor peptide V5, cell-permeable synthetic peptide inhibitor of Bax translocation to mitochondria; designed from Ku70, a protein that is suggested to suppress the mitochondrial translocation of Bax. Inhibits Bax-mediated apoptosis in vitro.

Cat. No.	Product Name	Water	DMSO	Ethanol
A11448	HA14-1	82 mg/mL (200.37 mM)	<1 mg/mL (<1 mM)	82 mg/mL (200.37 mM)
A10022	ABT-263 (Navitoclax)	100 mg/mL (102.6 mM)	<1 mg/mL (<1 mM)	<1 mg/mL (<1 mM)
A10255	ABT-737	100 mg/mL (122.93 mM)	<1 mg/mL (<1 mM)	<1 mg/mL (<1 mM)
A12907	BAM 7	2 mg/mL (4.93 mM)	<1 mg/mL (<1 mM)	<1 mg/mL (<1 mM)
A10955	TW-37	115 mg/mL (200.45 mM)	<1 mg/mL (<1 mM)	4 mg/mL (6.97 mM)
A10665	Obatoclax mesylate (GX15-070)	83 mg/mL (200.73 mM)	<1 mg/mL (<1 mM)	<1 mg/mL (<1 mM)
A14222	UMI-77	93 mg/mL (198.57 mM)	<1 mg/mL (<1 mM)	93 mg/mL heating (198.57 mM)
A13578	AT101 acetic acid	116 mg/mL (200.48 mM)	<1 mg/mL (<1 mM)	89 mg/mL (153.81 mM)
A12500	ABT-199 (Venetoclax)	100 mg/mL (115.14 mM)	<1 mg/mL (<1 mM)	<1 mg/mL (<1 mM)
A12823	Sabutoclax	100 mg/mL heating (142.69 mM)	<1 mg/mL (<1 mM)	54 mg/mL heating (77.05 mM)

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Bcl-2 Family

A10022 SALE

A10255 SALE

A13005

A12500 SALE

A10665 SALE

A16315

A11448 SALE

A14222 SALE

A15004

A12823

A13578

A16112

A16190

A10955

A16316

A12743

A16323

A14795

A16314

A16061 SALE

A15821

A15545

A13327

A12907 SALE

A13580

A16380

A16192

A15340

A15338

A15336

A15335

A11988 SALE

A15337 SALE

A15004

A15336

A15340

A15338

A15335

A11448

A10022

A10255

A12907

A10955

A10665

A14222

A13578

A12500

A12823

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