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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.

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ABT-737

Catalog No. A10255
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Bcl-2 抑制剂

ABT-737是一种类BH3抑制剂，能同时抑制Bcl-xL，Bcl-2和Bcl-w，EC50分别为78.7 nM，30.3 nM和197.8 nM;但对Mcl-1，Bcl-B及Bfl-1没有抑制作用。了解更多

Product Citations (15)

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- Jung Mo Lee, .et al. ABT-737, a BH3 Mimetic, Enhances the Therapeutic Effects of Ionizing Radiation in K-ras Mutant Non-Small Cell Lung Cancer Preclinical Model, Yonsei Med J, 2022, Jan;63(1):16-25 PMID: 34913280
- AidaVarela-Moreira, .et al. Utilizing in vitro drug release assays to predict in vivo drug retention in micelles, Int J Pharm, 2022, Apr 25;618:121638 PMID: 35257802
- Daniel F R Boehmer, .et al. OAS1/RNase L executes RIG-I ligand-dependent tumor cell apoptosis, Sci Immunol, 2021, Jul 16;6(61) PMID: 34272227
- Shivani Arora, .et al. Invariant natural killer T cells coordinate removal of senescent cells, Med, 2021, 2,1-13
- Ying Ji, .et al. Use of ratiometrically designed nanocarrier targeting CDK4/6 and autophagy pathways for effective pancreatic cancer treatment, Nat Commun, 2020, Aug 25;11(1):4249 PMID: 32843618
- Birgit Ritschka, .et al. The senotherapeutic drug ABT-737 disrupts aberrant p21 expression to restore liver regeneration in adult mice, Genes Dev, 2020, Apr 1;34(7-8):489-494 PMID: 32139422
- Hiroki Akiyama, .et al. Inhibition of USP9X Downregulates JAK2-V617F and Induces Apoptosis Synergistically With BH3 Mimetics Preferentially in Ruxolitinib-Persistent JAK2-V617F-Positive Leukemic Cells, Cancers, 2020, 12 (2) PMID: 32050632
- Hsu CC, .et al. α7-Nicotine acetylcholine receptor mediated nicotine induced cell survival and cisplatin resistance in oral cancer, Arch Oral Biol, 2020, Mar;111:104653 PMID: 31935534
- Gupta VK, .et al. Lysophosphatidic acid promotes survival of T lymphoma cells by altering apoptosis and glucose metabolism, Apoptosis, 2020, Feb;25(1-2):135-150 PMID: 31867678
- 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
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(+)-Apogossypol

Catalog No. A16316
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Bcl-2 family 抑制剂

(+)-Apogossypol是Bcl-2家族蛋白的有效抑制剂。与Bcl-2，Bcl-XL，Mcl-1，Bcl-W和Bcl-B上的BH3肽结合位点竞争，但与Bfl-1竞争，IC50为0.5至2μM。了解更多

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Gambogic acid

Catalog No. A11988
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Bcl-2 抑制剂

Gambogic acid是从藤黄汉树中分离出的天然产物。藤黄酸激活半胱氨酸蛋白酶，EC50为0.78-1.64μM，并竞争性抑制Bcl-XL，Bcl-2，Bcl-W，Bcl-B，Bfl-1和Mcl-1，IC50为1.47、1.21、2.02、0.66、1.06和分别为0.79μM。了解更多

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