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
- 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.
- 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。
- GC33247 AZD-5991 An Mcl-1 inhibitor
- 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。
- 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。 MCL1-IN-2对Metallo-&7#8946; -lactamases NDM-1,IMP-4,IMIS和L1的IC50S是0.4637 #956; M,M,3.980 &###&&7778777878787878787878787878787878787878787787877年7月778.7887;offlineefficient_models_2022q2.md -
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
- 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
- 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
- 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
- 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。
- 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
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GC11921
WEHI-539
WEHI539,WEHI 539
A selective Bcl-xL inhibitor -
GC12139
Gambogic Acid
藤黄酸; Beta-Guttiferrin
Gambogic Acid 是一种细胞渗透性 caspase 激活剂和细胞凋亡诱导剂,常用于乳腺癌、肺癌和肝癌等的研究。 -
GC13065
Chelerythrine Chloride
盐酸白屈菜红碱
Potent inhibitor of PKC and Bcl-xL -
GC12053
BAM7
BAM 7;BAM-7
A direct activator of Bax -
GC11106
AT-101
(-)-棉子素,(R)-(-)-Gossypol;R-(-)-gossypol acetic acid;AT 101;AT101
AT-101 (AT-101) 是天然产物棉酚的左旋异构体。 AT-101 与 Bcl-2、Mcl-1 和 Bcl-xL 蛋白结合,Kis 分别为 260±30 nM、170±10 nM 和 480±40 nM。 -
GC10153
Sabutoclax
BI-97C1
A pan-Bcl-2 inhibitor -
GC14080
Apogossypolone (ApoG2)
ApoG2
Apogossypolone (ApoG2) (ApoG2) 是一种具有口服活性的 Bcl-2 家族蛋白抑制剂,对 Bcl-2、Mcl-1 和 Bcl-XL 的 Ki 值分别为 35、25 和 660 nM。 -
GC11569
Obatoclax mesylate (GX15-070)
Obatoclax甲磺酸盐,GX15-070 Mesylate
An antagonist of pro-survival Bcl-2 proteins - GC13498 BM-1074 BM-1074 是一种有效且特异性的 Bcl-2/Bcl-xL 抑制剂,对 Bcl-2 和 Bcl-xL 的 Ki 值 < 1 nM,IC50 值分别为 1.8 nM 和 6.9 nM。 BM-1074 诱导细胞凋亡,并对四种小细胞肺癌细胞系(H146、H1963、H187 和 H1417)具有抗增殖活性,IC50 值为 1-2 nM。
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GC12649
TW-37
N-[4-(2-叔丁基苯磺酰基)苯基]-2,3,4-三羟基-5-(2-异丙基苯基甲基)苯甲酰胺,TW37,TW 37
An inhibitor of the Bcl-2 family proteins -
GC12405
ABT-263 (Navitoclax)
Navitoclax,ABT-263,ABT263,ABT 263
ABT-263 (Navitoclax) 是 Bcl-xL、Bcl-2 和 Bcl-w 的抑制剂,Ki 分别≤0.5 nM、≤1 nM 和≤1 nM。 -
GC17234
ABT-737
ABT 737, ABT737
An inhibitor of anti-apoptotic Bcl-2 proteins -
GC14069
ABT-199
维奈妥拉; ABT-199; GDC-0199; Venetoclax
Venetoclax (ABT-199, GDC-0199) 是 Bcl-2 的选择性抑制剂,在无细胞试验中 K i 为 0.01 nM。 -
GN10082
Gossypol
棉酚; BL 193
A natural polyphenol with diverse effects