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

Bcl-2 Family (Bcl-2蛋白家族)

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.

Bcl-2 Family 亚型特异性产品:

  • Bcl-2

  • Bcl-xL

  • Bcl-W

  • Mcl-1

  • Bfl-1

  • Bcl-B

  • Bax

  • Bak

  • Bim

目录号 产品名 作用方式 纯度
  • HY-15531
    Venetoclax Inhibitor ≥98.0%
    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 ≥98.0%
    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 ≥98.0%
    S63845 是一种有效的选择性骨髓细胞白血病 1 (MCL1) 抑制剂,结合人 MCL1Kd 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 99.65%
    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-138697
    S65487 Inhibitor 99.10%
    S65487 (VOB560) 是一种有效的选择性 Bcl-2 抑制剂。 S65487 对 BCL-2 突变也有活性,例如 G101V 和 D103Y。S65487 对 MCL-1,BFL-1 和 BCL-XL 的亲和力较差。S65487 诱导细胞凋亡 (apoptosis) 并具有抗癌活性。
  • HY-109184
    Murizatoclax Inhibitor
    Murizatoclax (AMG 397) 是一种有效,选择性和具有口服活性的髓样白血病 1 (MCL-1) 抑制剂,Ki 值为 15 pM。Murizatoclax 与促凋亡 BCL-2 家族成员竞争性结合 MCL1 的 BH3 结合沟。Murizatoclax 可用于癌症的研究。
  • HY-109185
    Pelcitoclax Inhibitor
    Pelcitoclax (APG-1252) 是一种有效的 Bcl-2/Bcl-xl 抑制剂,具有抗肿瘤和促凋亡作用。
  • 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-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-114855
    BT2 Inhibitor 99.56%
    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-112218
    MIK665 Inhibitor ≥98.0%
    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-101565
    Tapotoclax Inhibitor ≥99.0%
    Tapotoclax (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-10969
    Obatoclax Mesylate Inhibitor ≥98.0%
    Obatoclax Mesylate (GX15-070 Mesylate) 是 BH3 模拟物,是泛 BCL-2 家族蛋白抑制剂,对 BCL-2 的 Ki 值为 220 nM。Obatoclax Mesylate 诱导自噬 (autophagy) 依赖性细胞死亡,并靶向细胞周期蛋白 D1 进行蛋白酶体降解。Obatoclax Mesylate 具有抗癌和广谱抗寄生虫 (antiparasitic) 活性。
  • HY-P0081
    Bax inhibitor peptide V5 Inhibitor 98.12%
    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-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-108705
    BI-3802 Inhibitor 99.68%
    BI-3802 是一种高效的 BCL6 降解剂,能够抑制 BCL6 的Bric-à-brac (BTB) 结构域,IC50 值 ≤3 nM。BI-3802 可诱导 BCL6 蛋白聚集,并促进 E3 连接酶 SIAH1 介导的蛋白降解。BI-3802 具有抗肿瘤活性。
  • HY-12048
    Chelerythrine chloride Inhibitor ≥98.0%
    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-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。A-1210477 特异性结合 MCL-1,并以 MCL-1 依赖性方式促进癌细胞凋亡 (apoptosis)。
  • HY-112416
    AZD4320 Inhibitor 99.10%
    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 26 nM,17 nM,和 170 nM。

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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