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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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Muristerone A

Catalog No. A15340
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EcR 激动剂

Muristerone A是蜕皮激素的植物蜕皮激素类固醇类似物，可在哺乳动物细胞中诱导基因并在野生型Bax转染的细胞中引起细胞凋亡。了解更多

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Pyridoclax (MR-29072)

Catalog No. A16380
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Mcl-1 抑制剂

Pyridoclax是一种有效的Mcl-1抑制剂，Kd值为25 nM。了解更多

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Bax inhibitor peptide, negative control

Catalog No. A15338
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Bax 抑制剂

Bax inhibitor peptide，V5和P5的阴性对照，阴性对照肽，在体外抑制Bax易位至线粒体和Bax介导的细胞凋亡。了解更多

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Bax inhibitor peptide V5

Catalog No. A15337
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Bax 抑制剂

Bax inhibitor peptide V5，Bax易位至线粒体的细胞渗透性合成肽抑制剂；由Ku70设计的一种蛋白质，被认为可抑制Bax的线粒体易位。在体外抑制Bax介导的细胞凋亡。了解更多

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Bax inhibitor peptide P5

Catalog No. A15336
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Bax 抑制剂

Bax inhibitor peptide P5，Bax易位至线粒体的细胞渗透性合成肽抑制剂；由Ku70设计的一种蛋白质，被认为可抑制Bax的线粒体易位。在体外抑制Bax介导的细胞凋亡。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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Bax channel blocker

Catalog No. A15335
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Bax channel blocker

Bax channel blocker是Bax介导的线粒体细胞色素C释放的有效抑制剂（IC50 = 0.52μM）。了解更多

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CID5721353

Catalog No. A16192
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BCL6 抑制剂

CID5721353是B细胞淋巴瘤6抑制剂（BCL6抑制剂）。了解更多

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A-1210477

Catalog No. A15545
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MCL-1 抑制剂

A-1210477是有效的选择性MCL-1抑制剂。A-1210477诱导内在凋亡的标志，并证明了多发性骨髓瘤和非小细胞肺癌细胞系的单药杀伤。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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BDA-366

Catalog No. A15821
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Bcl-2 拮抗剂

BDA-366选择性抑制BCL2，将其转化为细胞死亡诱导剂。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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Acetate gossypol

Catalog No. A14795
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Bcl-2 抑制剂

Acetate gossypol是一种从棉籽中分离出来的多酚化合物，可通过模仿BH3来抑制Bcl-2。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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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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(+)-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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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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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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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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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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UMI-77

Catalog No. A14222
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Mcl-1 抑制剂

UMI-77是一种选择性的Mcl-1抑制剂，Ki为490 nM，显示出对Bcl-2家族其他成员的选择性。了解更多

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HA14-1

Catalog No. A11448
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Bcl-2 抑制剂

HA14-1与Bcl-2相互作用，抑制Bcl-2的抗凋亡作用。了解更多

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AZD5991

Catalog No. A16880
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Mcl-1 抑制剂

AZD-5991是一种有效的选择性Mcl-1抑制剂，在FRET分析中的IC50为0.7 nM，在表面等离子体共振（SPR）分析中的Kd为0.17 nM。了解更多

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BTSA1

Catalog No. A16835
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Bcl-2 modulator

BTSA1是经过药理优化的BAX激活剂，可与N末端激活位点高亲和力和特异性结合，并诱导BAX发生构象变化，从而导致BAX介导的细胞凋亡。它有效促进白血病细胞系和患者样品中的细胞凋亡，同时保留健康细胞。了解更多

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A-385358

Catalog No. A17064
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Bcl-XL 抑制剂

A-385358是Bcl-XL的抑制剂，可增强多种肿瘤细胞系中多种化学治疗剂（紫杉醇，依托泊苷，顺铂和阿霉素）的体外细胞毒活性。了解更多

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AZD-4320

Catalog No. A17171
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Bcl-2/Bcl-XL 抑制剂

AZD-4320是BH3模拟物和双重Bcl-2/Bcl-XL抑制剂。AZD4320 对于 KPUM-MS3，KPUM-UH1，和 STR-428 细胞系的 IC50 分别为 26 nM，17 nM，和 170 nM。了解更多

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Maritoclax (Marinopyrrole A)

Catalog No. A17206
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Mcl-1 抑制剂

Marinopyrrole A，也称为Maritoclax，是Mcl-1的选择性抑制剂，IC50值为10.1μM。了解更多

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BM 957

Catalog No. A18387
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Bcl-2 and Bcl-xL 抑制剂

BM 957 is a potent Bcl-2 and Bcl-xL inhibitor, with Kis of 1.2, <1 nM and IC50s of 5.4, 6.0 nM respectively. 了解更多

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MCL-1/BCL-2-IN-3

Catalog No. A18385
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Mcl-1 and Bcl-2 dual 抑制剂

MCL-1/BCL-2-IN-3 (Compound 2) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor with IC50s of 5.95 and 4.78 μM, respectively. 了解更多

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MCL-1/BCL-2-IN-4

Catalog No. A18380
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Mcl-1 and Bcl-2 dual 抑制剂

MCL-1/BCL-2-IN-4 (Compound 7) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor. 了解更多

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ML311

Catalog No. A18364
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Mcl-1/Bim interaction 抑制剂

ML311 is a potent and selective inhibitor of the Mcl-1/Bim interaction 了解更多

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S55746

Catalog No. A18361
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BCL-2 抑制剂

S55746 (BLC201) is a potent, orally active and selective BCL-2 inhibitor, with a Ki of 1.3 nM and a Kd of 3.9 nM. S55746 (BLC201) has antitumor activity with low toxicity. 了解更多

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Bax-activator-106

Catalog No. A18406
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Bax agonist

Bax-activator-106 is a specific Bax agonist. It acts by promoting Bax-dependent but not Bak-dependent apoptosis. 了解更多

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WEHI539

Catalog No. A13005
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Bcl-XL 抑制剂

WEHI539是Bcl-XL的选择性抑制剂，IC50为1.1 nM。了解更多

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Jaceosidin

Catalog No. A12080
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Jaceosidin是一种来源于艾蒿的药理活性黄酮，通过阻断培养的人乳腺上皮细胞中erk-1和-2的磷酸化来抑制佛波酯诱导的cox-2和MMP-9的上调。了解更多

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MIM1

Catalog No. A16315
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Mcl-1 抑制剂

MIM1是Mcl-1（IC50 = 4.8μM）的选择性小分子抑制剂，可克服Mcl-1依赖性白血病细胞的存活。了解更多

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- 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.
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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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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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BAM 7

Catalog No. A12907
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Bax activator

BAM 7使用FITC-BIM SAHB和BAX在竞争性FP分析中测得的EC50?3.3 μM结合BAX触发位点。了解更多

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- Takino JI, .et al. The inhibition of Bax activation-induced apoptosis by RasGRP2 via R-Ras-PI3K-Akt signaling pathway in the endothelial cells, Sci Rep, 2019, Nov 13;9(1):16717 PMID: 31723205
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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

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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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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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Obatoclax mesylate (GX15-070)

Catalog No. A10665
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Bcl-2 抑制剂

Obatoclax Mesylate (GX15-070)是一种Bcl-2拮抗剂，拮抗所有抗凋亡Bcl-2家族蛋白（平均IC50，3 umol/L），包括Mcl-1（IC50，2.9 umol/L）和Bfl-1（IC50，5 umol/L）。了解更多

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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
- Silva S, .et al. A diarylamine derived from anthranilic acid inhibits ZIKV replication, Sci Rep, 2019, Nov 27;9(1):17703 PMID: 31776405
- 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
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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

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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-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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