1. Apoptosis
  2. 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.

View Bcl-2 Family Pathway Map

Bcl-2 Family Related Products (45):

Cat. No. Product Name Effect Purity
  • HY-15531
    ABT-199 Inhibitor 99.80%
    ABT-199 is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM.
  • HY-10087
    Navitoclax Inhibitor 99.80%
    Navitoclax (ABT-263) is a potent and oral Bcl-2 family protein inhibitor that binds to multiple anti-apoptotic Bcl-2 family proteins, such as Bcl-xL, Bcl-2 and Bcl-w, with a Ki of less than 1 nM.
  • HY-100741
    S63845 Inhibitor 99.85%
    S63845 is a potent and selective myeloid cell leukemia 1 (MCL1) inhibitor with a Kd of 0.19 nM for human MCL1.
  • HY-50907
    ABT-737 Inhibitor 98.38%
    ABT-737 is a selective and BH3 mimetic Bcl-xLBcl-2 and Bcl-w inhibitor with EC50s of 78.7 nM, 30.3 nM and 197.8 nM, respectively.
  • HY-12468
    A-1210477 Inhibitor 98.89%
    A-1210477 is a potent and selective inhibitor of MCL-1 with a Ki of 0.45 nM.
  • HY-112416
    AZD4320 Inhibitor
    AZD4320 is a novel BH3-mimicking dual BCL2/BCLxL inhibitor with IC50s of 26 nM, 17 nM, and 170 nM for KPUM-MS3, KPUM-UH1, and STR-428 cells, respectively.
  • HY-112859
    VU0661013 Inhibitor
    VU661013 is a potent and selective MCL-1 inhibitor.
  • HY-101778
    ML311 Inhibitor
    ML311 is a potent and selective inhibitor of the Mcl-1/Bim interaction.
  • HY-10969
    Obatoclax Antagonist 99.20%
    Obatoclax is an antagonist of the BCL-2 family proteins. It binds to BCL-2 with a Ki of 220 nM.
  • HY-19725
    A-1155463 Inhibitor 98.55%
    A-1155463 is a highly potent and selective BCL-XL inhibitor with a EC50 value of 70 nM in Molt-4 cell.
  • HY-15607A
    WEHI-539 hydrochloride Inhibitor
    WEHI-539 hydrochloride is a selective inhibitor of Bcl-XL with IC50 of 1.1 nM.
  • HY-19741
    A-1331852 Inhibitor 99.21%
    A-1331852 is an orally available BCL-XL selective inhibitor with a Ki of less than 10 pM.
  • HY-P0081
    Bax inhibitor peptide V5 Inhibitor 99.79%
    Bax inhibitor peptide V5 is a Bax-mediated apoptosis inhibitor, used for cancer treatment. Sequence: Val-Pro-Met-Leu-Lys.
  • HY-N0087
    Gambogic Acid Inhibitor
    Gambogic acid is derived from the gamboges resin of the tree Garcinia hanburyi. Gambogic acid inhibits Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50s of 1.47 μM, 1.21 μM, 2.02 μM, 0.66 μM, 1.06 μM and 0.79 μM.
  • HY-102027
    FX1 Inhibitor >98.0%
    FX1 is a potent and specific BCL6 inhibitor, with an IC50 of around 35 μM.
  • HY-18628
    UMI-77 Inhibitor 98.04%
    UMI-77 is a selective Mcl-1 inhibitor, which shows high binding affinity to Mcl-1 (IC50=0.31 μM). UMI-77 binds to the BH3 binding groove of Mcl-1 with Ki of 490 nM, showing selectivity over other members of anti-apoptotic Bcl-2 members.
  • HY-17510
    Gossypol acetic acid Inhibitor 99.42%
    Gossypol, a natural product isolated from cottonseeds and roots, binds to Bcl-xL protein and Bcl-2 protein with Kis of 0.5-0.6 μM and 0.2-0.3 mM, respectively.
  • HY-15464A
    AT-101 acetic acid Inhibitor
    AT-101 acetic acid is the levorotatory isomer of a natural product Gossypol. AT-101 is determined to bind to Bcl-2, Mcl-1 and Bcl-xL proteins with Kis of 260±30 nM, 170±10 nM, and 480±40 nM, respectively.
  • HY-12011
    HA14-1 Inhibitor >98.0%
    HA14-1 is a Bcl-2/Bcl-XL antagonist. HA14-1 binds the designated pocket on Bcl-2 with the IC50 of ≈9 μM in competing with the Bcl-2 binding of Flu-BakBH3, and inhibits its function.
  • HY-12020
    TW-37 Inhibitor 98.50%
    TW-37 is a potent Bcl-2 inhibitor with Ki values of 260, 290 and 1110 nM for Mcl-1, Bcl-2 and Bcl-xL, respectively.
bcl-2-family-map.png

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.

Isoform Specific Products

Your Search Returned No Results.

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

Please try each isoform separately.