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 Isoform Specific Products:

  • Bcl-2

  • Bcl-xL

  • Bcl-W

  • Mcl-1

  • Bfl-1

  • Bcl-B

  • Bax

  • Bak

  • Bim

Cat. No. Product Name Effect Purity
  • 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-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-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-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-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-N0674A
    Dehydrocorydaline chloride Modulator 98.64%
    Dehydrocorydaline chloride (13-Methylpalmatine chloride) 是从中药延胡索 Corydalis yanhusuo 中分离得到的一种生物碱。Dehydrocorydaline 调节 BaxBcl-2 蛋白表达;激活 caspase-7caspase-8,并使 PARP 失活。Dehydrocorydaline chloride 能增强 p38 MAPK 活化,具有抗炎、抗癌等功效。。Dehydrocorydaline chloride 具有强大的抗疟疾作用,并具低细胞毒性 (细胞生存力> 90%), P. falciparum 3D7 strain (IC50=38 nM)。
  • HY-103269
    BAI1 Inhibitor 99.72%
    BAI1 是一种选择性的凋亡因子 BAX 变构抑制剂。BAI1 结合 BAX 并变构抑制其激活。BAI1 具有潜力用于 BAX 依赖性细胞死亡介导的疾病的研究。
  • 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。
  • HY-17510
    Gossypol (acetic acid) Inhibitor 99.41%
    Gossypol acetic acid ((±)-Gossypol-acetic acid) 是一种从棉籽和根中分离出来的天然产物,分别与 Bcl-xL 蛋白和 Bcl-2 蛋白结合,Ki 值分别为 0.5-0.6 μM 和 0.2-0.3 mM。
  • HY-13407
    Gossypol Antagonist 99.56%
    Gossypol 是一种从棉籽和根中分离出来的天然产物,分别与 Bcl-xL 蛋白和 Bcl-2 蛋白结合,Ki 值分别为 0.5-0.6 μM 和 0.2-0.3 mM。
  • HY-111381
    BI-3812 Inhibitor 99.35%
    BI-3812 是一种高效的 BCL6 抑制剂,能够抑制 BCL6 的 BTB 结构域,IC50 值 ≤3 nM,具有抗肿瘤活性。
  • HY-N0674
    Dehydrocorydaline Modulator ≥99.0%
    Dehydrocorydaline (13-Methylpalmatine) 是从中药延胡索 Corydalis yanhusuo 中分离得到的一种生物碱。Dehydrocorydaline 调节 BaxBcl-2 蛋白表达;激活 caspase-7caspase-8,并使 PARP 失活。Dehydrocorydaline 能增强 p38 MAPK 活化,具有抗炎、抗癌等功效。。Dehydrocorydaline 具有强大的抗疟疾作用,并具低细胞毒性 (细胞生存力> 90%), P. falciparum 3D7 strain (IC50=38 nM)。
  • HY-118341
    Clitocine Inhibitor
    Clitocine 是一种来源于蘑菇的腺苷核苷类似物,是一种有效的通读剂 (readthrough)。Clitocine 作为一种无义突变 (nonsense mutations) 的抑制剂,可诱导携带 p53 无义突变等位基因的细胞产生 p53 蛋白。Clitocine 可通过靶向 Mcl-1 诱导多药耐药肿瘤细胞凋亡。具有抗癌活性。
  • HY-15464A
    (R)-(-)-Gossypol acetic acid Inhibitor 98.02%
    (R)-(-)-Gossypol acetic acid (AT-101 (acetic acid)) 是天然产物 Gossypol 的左旋异构体。AT-101 结合到 Bcl-2Mcl-1Bcl-xL 蛋白,Ki 值分别为 260±30 nM,170±10 nM 和 480±40 nM。
  • HY-16695
    MIM1 Inhibitor ≥98.0%
    MIM-1 是一种骨髓细胞因子 1 (Mcl-1) 抑制剂。
  • HY-12020
    TW-37 Inhibitor 99.27%
    TW-37 是一种有效的 Bcl-2 抑制剂,作用于 Mcl-1Bcl-2Bcl-xLKi 值分别为 260,290 和 1110 nM。
  • HY-N0831
    Jaceosidin Activator 99.99%
    Jaceosidin 是从 Artemisia vestita 中得到的黄酮类化合物,可激活 Bax,下调 Mcl-1 和 c-FLIP 的表达,诱导癌细胞凋亡。Jaceosidin 具有抗癌和抗炎作用,能够降低炎性因子水平,激活 NF-κB,抑制 COX-2 的表达。
  • HY-N2897
    Dihydrokaempferol Inhibitor 99.02%
    Dihydrokaempferol 是从紫荆花 Bauhinia championii (Benth) 中分离得到的。 Dihydrokaempferol 诱导 apoptosis 并抑制 Bcl-2 和 Bcl-xL 的表达。Dihydrokaempferol 可以作为抗关节炎新药的良好候选。
  • HY-N0060B
    (E)-Ferulic acid Activator 99.20%
    (E)-Ferulic acid 是阿魏酸 (Ferulic acid) 的异构体,阿魏酸是芳香族化合物,在植物细胞壁中丰富。 (E)-Ferulic acid 引起 β-连环蛋白 (β-catenin) 的磷酸化,导致蛋白酶体降解,增加促凋亡因子 Bax 的表达并降低促存活因子存活蛋白的表达。(E)-Ferulic acid 可以有效去除活性氧 (ROS) 和抑制脂质过氧化。(E)-Ferulic acid 在人肺癌细胞系 H1299 中发挥抗增殖和抗迁移作用。
  • HY-N3584
    Paris saponin VII Inhibitor ≥99.0%
    Paris saponin VII (Chonglou Saponin VII) 是从延龄草 (Trillium tschonoskii Maxim) 的根和根茎中分离的甾体皂苷。Paris saponin VII 诱导的 K562/ADR 细胞凋亡与 Akt/p38 MAPKP-gp 的抑制有关。Paris saponin VII 减弱线粒体膜电位,增加凋亡相关蛋白 (Bax 和细胞色素 c) 的表达,并降低 Bcl-2caspase-9caspase-3PARP-1p-Akt 的蛋白表达水平。Paris saponin VII 在 K562/ADR 细胞中诱导强烈的自噬,可用于白血病的研究。

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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