1. Signaling Pathways
  2. Apoptosis
  3. Bcl-2 Family

Bcl-2 Family

Bcl-2 is a family of evolutionarily related proteins. These proteins govern mitochondrial outer membrane permeabilization (MOMP) and can be either pro-apoptotic (Bax, Bad, Bak and Bok among others) or anti-apoptotic (including Bcl-2 proper, Bcl-xL, and Bcl-w, among an assortment of others). There are a total of 25 genes in the Bcl-2 family known to date. Human genes encoding proteins that belong to this family include: Bak1, Bax, Bal-2, Bok, Mcl-1.

Cat. No. Product Name Effect Purity
  • HY-15531
    Venetoclax Inhibitor 99.95%
    Venetoclax (ABT-199; GDC-0199) 是一种高效,有选择性和口服有效的 Bcl-2 抑制剂,Ki 小于0.01 nM。Venetoclax 可以诱导自噬 (autophagy) 作用。
  • HY-10087
    Navitoclax Inhibitor 99.97%
    Navitoclax (ABT-263) 是有效,可口服的 Bcl-2 抑制剂,可与Bcl-xL,Bcl-2, Bcl-w等多种Bcl-2家族蛋白结合,Ki 值小于 1 nM。
  • HY-100741
    S63845 Inhibitor 99.94%
    S63845是有效的选择性骨髓细胞白血病1 (MCL1) 抑制剂,结合人MCL1的Kd 值为0.19 nM。
  • HY-50907
    ABT-737 Inhibitor 99.59%
    ABT-737 是一种类似 BH3 的 Bcl-2Bcl-xL,和 Bcl-w 的抑制剂,EC50 值分别为 30.3 nM,78.7 nM 和 197.8 nM。
  • HY-19741
    A-1331852 Inhibitor 99.81%
    A-1331852是具有口服活性的BCL-XL选择性抑制剂,Ki值小于10 pM。
  • HY-114855
    BT2 Inhibitor 98.10%
    BT2 是 BCKDC 激酶 (BDK) 抑制剂,IC50 值为 3.19 μM。BT2 与 BDK 的结合会触发支链 α-酮酸脱氢酶复合物 (BCKDC) 的 N 末端结构域的螺旋运动,从而导致 BDK 与 BCKDC 分离。BT2 (compound 4) 也是一种有效的选择性的 Mcl-1 抑制剂,Ki 值为 59 μM。
  • HY-129681
    MCL-1/BCL-2-IN-1 Inhibitor 98.04%
    MCL-1/BCL-2-IN-2 (Compound Nap-1) 是一种有效的选择性 Mcl-1Bcl-2 抑制剂,IC50 分别为 4.45 和 3.18 μM。
  • HY-135273
    BCL2-IN-1
    BCL2-IN-1,一种有效的 Bcl-2 抑制剂,与 Bcl-2 结合,Ki 值 <0.01 nM。
  • HY-10969
    Obatoclax Mesylate Inhibitor 99.74%
    Obatoclax Mesylate 是 BCL-2 家族蛋白的抑制剂,与 BCL-2 结合的 Ki 为 220 nM。
  • HY-19725
    A-1155463 Inhibitor 99.62%
    A-1155463是高效选择性的 BCL-XL 抑制剂,在Molt-4细胞中的EC50值为70 nM。
  • HY-101565
    AMG-176 Inhibitor 99.53%
    AMG-176 是一种有效的、有口服活性的、骨髓细胞因子 1 (MCL-1) 的选择性抑制剂,其 Ki 值为 0.13 nM。
  • HY-101533
    AZD-5991 Inhibitor 99.50%
    AZD-5991 是一种有效的选择性 Mcl-1 抑制剂,FRET 实验检测的 IC50 为 0.7 nM, SPR 实验检测的 Kd 为 0.17 nM。
  • HY-15607A
    WEHI-539 hydrochloride Inhibitor 98.16%
    WEHI-539 hydrochloride 是一种选择性的 Bcl-XL 抑制剂,IC50 为 1.1 nM。
  • HY-12468
    A-1210477 Inhibitor 98.89%
    A-1210477 是一种有效,选择性的 MCL-1 抑制剂,Ki 值为 0.45 nM。
  • HY-12048
    Chelerythrine chloride Inhibitor 98.56%
    Chelerythrine chloride 是一种有效,可渗透细胞的蛋白酶 C (protein kinase C) 抑制剂,能够抑制 PKC 活性,IC50 值为 660 nM。Chelerythrine chloride 抑制 Bcl-XL-Bak BH3 肽结合,IC50 为 1.5 μM,并从 Bcl-XL 取代了 Bax。Chelerythrine chloride 诱导细胞凋亡 (apoptosis) 和自噬 (autophagy)。
  • HY-P0081
    Bax inhibitor peptide V5 Inhibitor 99.62%
    Bax inhibitor peptide V5 (BIP-V5) 是一种 Bax 诱导凋亡的抑制剂,主要用于癌症研究。
  • HY-112218
    MIK665 Inhibitor 98.40%
    MIK665 (S-64315) 是一种特异性的 Mcl-1 抑制剂,IC50 为 1.81 nM,详细信息请参考专利文献 WO2016207225A1 中的化合物 Preparation 13。
  • HY-117288
    S55746 Inhibitor 98.97%
    S55746 (BLC201) 是一种有效、可口服、选择性的 BCL-2 抑制剂,其 Ki 值和 Kd 值分别为 1.3 nM 和 3.9 nM。S55746 (BLC201) 具有抗肿瘤活性且毒性低。
  • HY-102027
    FX1 Inhibitor >98.0%
    FX1 是一种强效且特异性的 BCL6 抑制剂, IC50 大约为 35 μM。
  • HY-N0087
    Gambogic Acid Inhibitor
    Gambogic Acid (Beta-Guttiferrin) 来自 Garcinia hanburyi 树的藤黄树脂。Gambogic Acid (Beta-Guttiferrin) 抑制 Bcl-XLBcl-2Bcl-WBcl-BBfl-1Mcl-1IC50 分别为 1.47 μM,1.21 μM,2.02 μM,0.66 μM,1.06 μM 和 0.79 μM。

Bcl-2 family members have been grouped into three classes. The anti-apoptotic subfamily contains the Bcl-2, Bcl-XL, Bcl-w, Mcl-1, Bfl1/A-1, and Bcl-B proteins, which suppress apoptosis and contain all four Bcl-2 homology domains, designated BH1-4. The pro-apoptotic subfamily contain BH1-3 domains, such as Bax, Bak, and Bok. A third class of BH3 only proteins Bad, Bid, Bim, Noxa and Puma have a conserved BH3 domain that can bind and regulate the anti-apoptotic BCL-2 proteins to promote apoptosis [1].


The intrinsic pathway is initiated by various signals, principally extracellular stimuli. BH3-only proteins (Bim, Bid, Bad, Noxa, Puma) engage with anti-apoptotic Bcl-2 family proteins to relieve their inhibition of Bax and Bak to activate them. Next, Bax and Bak are oligomerized and activated, leading to mitochondrial outer membrane permeabilization. Once mitochondrial membranes are permeabilized, cytochrome c and/or Smac/DIABLO is released into the cytoplasm, wherein they combine with an adaptor molecule, Apaf-1, and an inactive initiator Caspase, Pro-caspase 9, within a multiprotein complex called the apoptosome. Smac/DIABLO inhibits IAPs to activate Caspase 9. Caspase 9 activates Caspase 3, which is the initiation step for the cascade of Caspase activation. The extrinsic pathway can be activated by cell surface receptors, such as Fas and TNF Receptor, subsequently activating Caspase 8, and leads to Caspase 3 activation and cell demolition. Caspases in turn cleave a series of substrates, activate DNases and orchestrate the demolition of the cell. Bcl-2 family proteins are also found on the endoplasmic reticulum and the perinuclear membrane in hematopoietic cells, but they are predominantly localized to mitochondria [2]

 

Reference:
[1]. Cotter TG, et al. Apoptosis and cancer: the genesis of a research field. Nat Rev Cancer. 2009 Jul;9(7):501-7.

[2]. Kang MH, et al. Bcl-2 inhibitors: targeting mitochondrial apoptotic pathways in cancer therapy. Clin Cancer Res. 2009 Feb 15;15(4):1126-32.

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