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-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-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-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-N6573
    Bufarenogin Activator
    Bufarenogin 可通过 BaxANT 诱导凋亡。
  • HY-118948
    MSN-50 Inhibitor
    MSN-50 是一种 BaxBak 寡聚抑制剂,能有效抑制脂质体的通透性,防止基因毒性细胞死亡,促进神经保护。
  • HY-129478
    TC11 Inhibitor 98.04%
    TC11 是一种 MCL1 降解剂和 Caspase-9CDK1 激活剂。TC11 作为苯酞酰亚胺衍生物在结构上与免疫调节药物有关。在长时间有丝分裂阻滞期间,TC11 诱导 MCL1 降解导致凋亡性死亡。
  • 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-N0674A
    Dehydrocorydaline chloride Modulator 98.64%
    Dehydrocorydaline chloride (13-Methylpalmatine chloride) 是一种生物碱。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-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-13407
    Gossypol Antagonist 99.56%
    Gossypol 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-N0674
    Dehydrocorydaline Modulator ≥99.0%
    Dehydrocorydaline (13-Methylpalmatine) 是一种生物碱。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-17510
    Gossypol (acetic acid) Inhibitor 99.41%
    Gossypol acetic acid ((±)-Gossypol-acetic acid) 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-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-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-125876
    PROTAC Bcl2 degrader-1 Inhibitor 98.28%
    PROTAC Bcl2 degrader-1 (Compound C5) 是一种 PROTAC,通过将 E3 连接酶 cereblon 的配体 pomalidomide 引入到 Mcl-1/Bcl-2 的双重抑制剂 Nap-1,来有效、特异性地诱导 Bcl-2 (IC50,4.94 μM;DC50,3.0 μM) 和 Mcl-1 (IC50,11.81 μM) 的降解。
  • 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-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。

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]


[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.

Isoform Specific Products

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.