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 Isoform Specific Products:

  • Bcl-2

  • Bcl-xL

  • Bcl-W

  • Mcl-1

  • Bfl-1

  • Bcl-B

  • Bax

  • Bak

  • Bim

Bcl-2 Family Related Products (41):

Cat. No. Product Name Effect Purity
  • HY-15531
    ABT-199 Inhibitor 99.80%
    ABT-199 is a highly potent, orally bioavailable and Bcl-2-selective inhibitor with Ki of <0.01 nM.
  • HY-10087
    Navitoclax Inhibitor 99.80%
    Navitoclax is a potent and orally bioavailable Bcl-2 family protein inhibitor that binds with high affinity (Ki < 1 nM) to multiple anti-apoptotic Bcl-2 family proteins including Bcl-xL, Bcl-2 and Bcl-w.
  • HY-100741
    S63845 Inhibitor 99.85%
    S63845 is a potent and selective myeloid cell leukemia 1 (MCL1) inhibitor; binds human MCL1 with a Kd of 0.19 nM.
  • HY-50907
    ABT-737 Inhibitor 98.38%
    ABT-737 is a BH3 mimetic inhibitor of Bcl-xLBcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively, and shows no inhibition against Mcl-1, Bcl-B or Bfl-1.
  • HY-12468
    A-1210477 Inhibitor 98.89%
    A-1210477 is a potent and selective inhibitor of MCL-1, and weakly binds to BCL-2 and BCL-XL, with Ki of 0.45 nM, 132 nM and >660 nM, respectively.
  • 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-15191
    Sabutoclax Inhibitor
    Sabutoclax is a potent and effective Bcl-2 Family (Bcl-2, Bcl-XL, Mcl-1, Bfl-1) inhibitor with IC50s of 0.32 μM, 0.31 μM, 0.20 μM, and 0.62 μM, respectively.
  • HY-111467
    Mcl1-IN-4 Inhibitor
    Mcl1-IN-4 is an inhibitor of Mcl1 with an IC50 of 0.2 μM.
  • HY-10969
    Obatoclax Antagonist 99.20%
    Obatoclax is a BCL-2 family antagonist, which binds this cytosolic form of BCL-2 with a Ki of ≈220 nM. Obatoclax inhibits this interaction for all BCL-XL, MCL-1, BCL-w, A1, and BCL-b (Ki≈1-7 μM).
  • HY-15607A
    WEHI-539 hydrochloride Inhibitor
    WEHI-539 hydrochloride is a selective inhibitor of Bcl-XL with IC50 of 1.1 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-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-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-102027
    FX1 Inhibitor >98.0%
    FX1 is a potent and specific BCL6 inhibitor, with an IC50 of around 35 μM.
  • 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

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