Bcl-2 Family(Bcl-2蛋白家族)
Bcl-2 family proteins are a group of proteins homologous to the Bcl-2 protein and characterized by containing at least one of four conserved Bcl-2 homology (BH) domains (BH1, BH2, BH3 and BH4). Bcl-2 family proteins, consisting of pro-apoptotic and anti-apoptotic molecules, can be classified into the following three subfamilies according to sequence homology within four BH domains: (1) a subfamily shares sequence homology within all four BH domains, such as Bcl-2, Bcl-XL and Bcl-w which are anti-apoptotic; (2) a subfamily shares sequence homology within BH1, BH2 and BH4, such as Bax and Bak which are pro-apoptotic; (3) a subfamily shares sequence homology only within BH3, such as Bik and Bid which are pro-apoptotic.
Products for Bcl-2 Family
- Cat.No. 产品名称 Information
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GC36558
Mcl1-IN-12
Mcl1-IN-12 (Compound F) 是一种选择性的 Mcl-1 抑制剂,对 Bcl-2 的作用较弱,Ki 值分别为 0.29 和 3.1 μM。
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GC36557
Mcl1-IN-11
Mcl1-IN-11 (Compound G) 是一种选择性的 Mcl-1 抑制剂,对 Bcl-2 的作用较弱,Ki 值分别为 0.06 和 4.2 μM。
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GC36556
Mcl1-IN-1
2-[2-[(5-氯-8-羟基-7-喹啉基)(2-吡啶基氨基)甲基]苯氧基]乙酸
Mcl1-IN-1 是一种骨髓细胞因子 1 (Mcl-1) 抑制剂,IC50 为 2.4 ?M。 -
GC35882
dMCL1-2
dMCL1-2 是一种基于 PROTAC 技术的,高效、选择性的 MCL1 降解剂,结合 MCL1 的 KD 值为 30 nM。dMCL1-2 通过降解 MCL1 激活细胞凋亡。
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GC35001
(S)-Gossypol acetic acid
(S)-(+)-Gossypol acetic acid
(S)-Gossypol acetic acid 是天然产物 Gossypol 的异构体。(S)-Gossypol 以高亲和力结合到 Bcl-xL 和 Bcl-2 蛋白的 BH3 结合沟。 -
GC34980
(E)-Ferulic acid
反式阿魏酸,(E)-Coniferic acid
Trans-ferulic acid is a potent activator of AMPKunder high glucose condition. -
GC34389
PUMA BH3
PUMABH3是一种p53正向凋亡调控因子(PUMA)BH3结构域多肽,作为Bak的直接激活剂,Kd值为26nM。
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GC34263
Bak BH3
BakBH3是一种多肽,源于Bak蛋白的BH3结构域,在细胞中,能够抑制Bcl-xL的活性。
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GC34134
Glycocholic acid
甘氨胆酸
Glycocholic acid是一种参与脂肪乳化的结晶胆汁酸,是胆酸与甘氨酸的结合物,它以钠盐的形式存在于哺乳动物的胆汁中。 -
GC34096
(R)-(-)-Gossypol acetic acid (AT-101 (acetic acid))
(R)-(-)-醋酸棉酚; AT-101 (acetic acid); (-)-Gossypol acetic acid; (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 Ki 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. -
GC33407
BM 957
BM957是Bcl-2和Bcl-xL的有效抑制剂,其Ki值分别为1.2,<1nM,IC50值分别为5.4,6.0nM。
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GC33401
S55746 hydrochloride (BLC201 (hydrochloride))
BCL201 hydrochloride
S55746 hydrochloride (BLC201 (hydrochloride)) (BCL201 hydrochloride) 是一种有效的,具有口服活性的选择性 BCL-2 抑制剂,Ki 为 1.3 nM,Kd 为 3.9 nM。 S55746 hydrochloride (BLC201 (hydrochloride)) (BCL201 hydrochloride) 具有低毒的抗肿瘤活性。 -
GC33364
Mcl1-IN-4
Mcl1-IN-4是Mcl1的抑制剂,IC50值为0.2μM。
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GC33347
Mcl1-IN-3
Mcl1-IN-3是Mcl1的抑制剂,来自专利专利WO2015153959A2,化合物实例57;IC50和Ki值分别为0.67和0.13μM。
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GC33312
ML311
An Mcl-1 inhibitor
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GC33295
MIK665 (S-64315)
S-64315
An Mcl-1 inhibitor -
GC33283
AZD-5991 Racemate
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.
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GC33255
AZD4320
AZD4320是BH-3的新型类似物,有效的BCL2/BCLxL的双重抑制剂。AZD4320对于KPUM-MS3,KPUM-UH1,和STR-428细胞系的IC50分别为26nM,17nM,和170nM。
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GC33247
AZD-5991
An Mcl-1 inhibitor
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GC33239
AZD-5991 S-enantiomer
AZD-5991S-enantiomer是AZD-5991的低活性S型对映体。AZD-5991S-enantiomer是一种Mcl-1抑制剂,FRET实验检测的IC50为6.3μM,SPR实验检测的Kd为0.98μM。
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GC33052
VU0661013
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.
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GC33035
Mcl1-IN-2
7-[(2-吡啶基氨基)-2-噻吩基甲基]-8-喹啉醇
Mcl1-IN-2 是骨髓细胞因子 1 (Mcl-1) 的抑制剂。 Mcl1-IN-2 是一种非竞争性的德里 metallo-β-lactamase (NDM-1) 抑制剂。
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GC32998
Ginsenoside Rh4
人参皂苷RH4
Ginsenoside Rh4 is an important active ingredient of traditional Chinese medicine ginseng, which has been shown to inhibit Wnt/β-Catenin, JAK2/STAT3, TGF-β/Smad2/3 and other signaling pathways. -
GC32981
A-385358
A-385358是Bcl-XL的一个选择性抑制剂,对于Bcl-XL和Bcl-2的Ki值分别为0.80和67nM。
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GC32947
S55746 (BLC201)
BCL201
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. -
GC31806
Bz 423 (BZ48)
BZ48
Bz 423 (BZ48) 是一种促凋亡的 1,4-苯二氮卓类药物,在狼疮小鼠模型中具有治疗特性,显示出对自身反应性淋巴细胞的选择性,并激活 Bax 和 Bak。 -
GC19452
AMG-176
AMG-176
AMG-176 (Tapotoclax) 是一种有效的、选择性的、具有口服活性的 MCL-1 抑制剂,Ki 为 0.13 nM。 -
GC10661
Destruxin B
黑僵菌素 B
An insecticidal mycotoxin -
GC17513
A-1331852
A Bcl-xL inhibitor
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GC17512
A-1155463
醋酸艾塞那肽
A Bcl-xL inhibitor -
GC18136
BH3I-1
BHI1; BH 3I1
An inhibitor of anti-apoptotic Bcl-2 proteins -
GC12621
S63845
An Mcl-1 inhibitor
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GC16278
A-1210477
A selective Mcl-1 inhibitor
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GC10721
BDA-366
1-[[(2S)-3-(二乙基氨基)-2-羟基丙基]氨基]-4-[[(2S)-2-环氧乙烷基甲基]氨基]-9,10-蒽醌
A Bcl2-BH4 domain antagonist -
GC11140
Radotinib(IY-5511)
拉多替尼
A selective Bcr-Abl tyrosine kinase inhibitor -
GC17008
(+)-Apogossypol
變棉子酚,Apogossypol; NSC736630
(+)-Apogossypol 是一种泛 BCL-2 拮抗剂。 (+)-Apogossypol 与 Mcl-1、Bcl-2 和 Bcl-xL 结合,EC50 分别为 2.6、2.8 和 3.69 μM。
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GC12902
Pyridoclax
MR-29072
Pyridoclax 是一种潜在的 Mcl-1 抑制剂。 -
GC15805
UMI-77
A selective Mcl-1 inhibitor
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GC10567
TCPOBOP
An agonist for mouse CAR
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GC15480
Marinopyrrole A
Marinopyrrole A
An alkaloid with antibacterial activity -
GC13317
WEHI-539 hydrochloride
A selective Bcl-xL inhibitor
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GC16938
Muristerone A
米乐甾酮A
An ecdysteroid receptor agonist -
GC15400
MIM1
4-[[[2-(环己基亚氨基)-4-甲基-3(2H)-噻唑基]亚氨基]甲基]-1,2,3-苯三醇,Inhibitor of Mcl-1
An Mcl-1 inhibiting molecule -
GC12046
iMAC2
iMAC2 是一种有效的 MAC 抑制剂,IC50 为 28 nM,LD50 为 15000 nM。
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GC15987
BIM, Biotinylated
Bim peptide fragment with a biotin moiety attached
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GC16695
Bax inhibitor peptide, negative control
Peptide inhibit Bax translocation to mitochondria
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GC17195
Bax inhibitor peptide V5
BIP-V5; BAX Inhibiting Peptide V5
A Bax inhibitor -
GC16023
Bax inhibitor peptide P5
Bax inhibitor
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GC12763
Bax channel blocker
Bax 通道阻滞剂是 BAX(一种凋亡调节剂)的选择性变构抑制剂。 Bax 通道阻滞剂直接与 BAX 结合并变构抑制 BAX 活化。 Bax 通道阻滞剂具有研究由 BAX 依赖性细胞死亡介导的疾病的潜力。
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GC12258
2,3-DCPE hydrochloride
2,3-DCPE 是一种促凋亡化合物,对癌细胞\u003cem\u003e相对于\u003c/em\u003e正常人细胞具有选择性