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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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Sabutoclax

Catalog No. A12823
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Bcl-2 抑制剂

Sabutoclax (BI-97C1)是pan-Bcl-2抑制剂，包括Bcl-xL，Bcl-2，Mcl-1和Bfl-1，IC50分别为0.31 μM，0.32 μM，0.20 μM和0.62 μM。了解更多

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- 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
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Bcl-2 Inhibitor

Catalog No. A13580
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Bcl-2 抑制剂

Bcl-2 Inhibitor包含两种互变异构体的混合物。一种有效的，细胞可渗透的Bcl-2抑制剂与Bak BH3肽竞争体外结合Bcl-2和Bcl-XL的作用（分别为IC50 = 10 uM和7 uM）。了解更多

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- 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
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ABT-263 (Navitoclax)

Catalog No. A10022
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Bcl-2 抑制剂

ABT-263 (Navitoclax)是一种有效的Bcl-2家族抑制剂 (Bcl-2，Bcl-xL和Bcl-w的Ki <1 nmol/L)。ABT-263对Bcl- xL，Bcl-2和Bcl-w，( Ki≤1nmol/ L) 维持高亲和力，但与Mcl-1和A1的结合更弱。了解更多

Product Citations (20)

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- Rindert Missiaen, .et al. GCN2 inhibition sensitizes arginine-deprived hepatocellular carcinoma cells to senolytic treatment, Cell Metab, 2022, Aug 2;34(8):1151-1167 PMID: 35839757
- Ashlyn Parkhurst, .et al. Dual mTORC1/2 inhibition compromises cell defenses against exogenous stress potentiating Obatoclax-induced cytotoxicity in atypical teratoid/rhabdoid tumors, Cell Death Dis, 2022, Apr 28;13(4):410 PMID: 35484114
- Suzuki, Keiji, .et al. Characterization of radiation-induced micronuclei associated with premature senescence, and their selective removal by senolytic drug, ABT-263, Mutat Res Genet Toxicol Environ Mutagen, 2022, 876-877. 503448
- Rotem Ben-Hamo, .et al. Predicting and affecting response to cancer therapy based on pathway-level biomarkers, Nat Commun, 2020, 11: 3296
- Hua Xu, .et al. Preclinical Study Using ABT263 to Increase Enzalutamide Sensitivity to Suppress Prostate Cancer Progression Via Targeting BCL2/ROS/USP26 Axis Through Altering ARv7 Protein Degradation, Cancers (Basel), 2020, Apr; 12(4): 831 PMID: 32235588
- 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
- Stephanie Ketterer, .et al. Cathepsin D deficiency in mammary epithelium transiently stalls breast cancer by interference with mTORC1 signaling, Nat Commun, 2020, Oct 12;11(1):5133 PMID: 33046706
- Makoto Koyama, .et al. Low-dose trametinib and Bcl-xL antagonist have a specific antitumor effect in KRAS-mutated colorectal cancer cells, Int J Oncol, 2020, Sep 2 PMID: 32901840
- Min Li, .et al. Clearance of HIV infection by selective elimination of host cells capable of producing HIV, Nat Commun, 2020, 11: 4051 PMID: 32792548
- Hamzehlou S, .et al. Anti-tumor activity of neratinib, a pan-HER inhibitor, in gastric adenocarcinoma cells, Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- 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
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ABT-199 (Venetoclax)

Catalog No. A12500
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Bcl-2 抑制剂

ABT-199 (Venetoclax) 是一种所谓的BH3类似药物，旨在阻断Bcl 2蛋白的功能。了解更多

Product Citations (6)

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- Ashlyn Parkhurst, .et al. Dual mTORC1/2 inhibition compromises cell defenses against exogenous stress potentiating Obatoclax-induced cytotoxicity in atypical teratoid/rhabdoid tumors, Cell Death Dis, 2022, Apr 28;13(4):410 PMID: 35484114
- Anna L Koessinger, .et al. Increased apoptotic sensitivity of glioblastoma enables therapeutic targeting by BH3-mimetics, Cell Death Differ, 2022, Apr 26 PMID: 35473984
- Florian J Bock, .et al. Apoptotic stress-induced FGF signalling promotes non-cell autonomous resistance to cell death, Nat Commun, 2021, Nov 12;12(1):6572 PMID: 34772930
- 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
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A-1155463

Catalog No. A16112
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BCL-XL 抑制剂

A-1155463是一种高效且选择性强的BCL-XL抑制剂，A-1155463显示与BCL-XL的皮摩尔结合亲和力（Ki = <0.01 nM），与BCL-2的结合力弱1000倍以上（Ki = 80 nM）和相关蛋白BCL-W（Ki = 19 nM）和MCL-1（Ki> 440 nM）。了解更多

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- 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
- 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
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AT-101

Catalog No. A15004
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Bcl-2 抑制剂

(R)-(-)-Gossypol对映体AT101与Bcl-2，Bcl-xL和Mcl-1结合，Ki分别为0.32μM，0.48μM和0.18μM。了解更多

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A-1331852

Catalog No. A16190
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BCL-XL 抑制剂

A-1331852是有效的选择性BCL-XL抑制剂。BCL-XL是主要的抗凋亡生存蛋白，可能是CML中的新型治疗靶标。了解更多

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AT101 acetic acid

Catalog No. A13578
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pan Bcl-2 抑制剂

AT101 acetic acid对映体AT101与Bcl-2，Bcl-xL和Mcl-1结合，Ki分别为0.32μM，0.48μM和0.18μM；不抑制BIR3域和BID。了解更多

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TW-37

Catalog No. A10955
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Bcl-2 抑制剂

TW-37是Bcl-2的小分子抑制剂，可抑制胰腺癌细胞的生长，并通过一种涉及Notch-1和Jagged-1失活的新途径介导的胰腺癌细胞凋亡。了解更多

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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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BM-1074

Catalog No. A12743
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Bcl-2/Bcl-xL 抑制剂

BM-1074是有效且有效的Bcl-2/Bcl-xL抑制剂，Ki <1 nM。了解更多

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BH3I-1

Catalog No. A16061
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Bcl-XL 拮抗剂

BH3I-1是Bcl-XL-BH3 domain interaction抑制剂，Ki值为2.4 μM。它是一种Bcl-2家族蛋白的选择性抑制剂。了解更多

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(S)-Gossypol acetic acid

Catalog No. A16323
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Bcl-2 抑制剂

(S)-Gossypol acetic acid是Bcl-2的抑制剂，在过表达Bcl-2（IC50，18.1μM）或Bcl-xL（IC50，22.9μM）的Jurkat细胞中有效诱导细胞死亡。了解更多

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Apogossypolone (ApoG2)

Catalog No. A16314
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Bcl-2 抑制剂

Apogossypolone (ApoG2)是一种Bcl-2的非肽小分子抑制剂。了解更多

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WEHI-539 hydrochloride

Catalog No. A13327
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Bcl-xL 抑制剂

WEHI-539 hydrochloride是BCL-xL的小分子抑制剂，IC50值为1.1 nM。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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