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

Bcl-2 Family

Bcl-2 Family

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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 Family Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-15464
    (R)-(-)-Gossypol
    		Inhibitor 98.82%
    (R)-(-)-Gossypol (AT-101) 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.
    (R)-(-)-Gossypol
  • HY-118948
    MSN-50
    		Inhibitor 98.68%
    MSN-50 is a Bax and Bak oligomerization inhibitor. MSN-50 efficiently inhibits liposome permeabilization, prevents genotoxic cell death and promotes neuroprotection.
    MSN-50
  • HY-N6850
    Calenduloside E
    		99.07%
    Calenduloside E is a pentacyclic triterpenoid saponin that can be extracted from the bark and roots of Aralia ovata, and has anti-inflammatory and anti-apoptotic activities. Calenduloside E alleviates atherosclerosis by regulating macrophage polarization, improves mitochondrial function by regulating the AMPK-SIRT3 pathway, and alleviates acute liver injury. In addition, Calenduloside E promotes the interaction between L-type calcium channels and Bcl-2 related apoptosis genes, inhibits calcium overload, and alleviates myocardial ischemia/reperfusion injury. Calenduloside E also improves non-alcoholic fatty liver disease by regulating heat shock-dependent pathways, and inhibits ROS mediated JAK1-STAT3 pathways to reduce cellular inflammatory responses.
    Calenduloside E
  • HY-N3001
    Isolinderalactone
    		Inhibitor 98.79%
    Isolinderalactone suppresses human glioblastoma growth and angiogenic activity through the inhibition of VEGFR2/KDR/Flk-1 activation in endothelial cells. Isolinderalactone suppresses the expression of B-cell lymphoma 2 (Bcl-2), survi
    Isolinderalactone
  • 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.
    HA14-1
  • HY-12286
    PI-1840
    		Modulator 98.78%
    PI-1840 is a potent and selective chymotrypsin-like (CT-L) inhibitor for with an IC50 value of 27 nM. PI-1840 inhibits cell proliferation and arrest cell cycle at G2/M phase. PI-1840 induces apoptosis and induces autophagy. PI-1840 induces the accumulation of proteasome substrates p27, Bax, and IκB-α.
    PI-1840
  • HY-119402
    TP-021
    		Inhibitor 99.14%
    TP-021 (BCL6-IN-8c) is a potent and orally active B-cell lymphoma 6 (BCL6)-corepressor interaction inhibitor with an IC50 of 0.10 µM in cell-free enzyme-linked immunosorbent assay.
    TP-021
  • HY-101778
    ML311
    		Inhibitor 98.98%
    ML311 is a potent and selective inhibitor of the Mcl-1/Bim interaction.
    ML311
  • HY-B0862
    Pendimethalin
    		Inhibitor 99.75%
    Pendimethalin is an orally active herbicide that controls annual grasses and certain broadleaf weeds. Pendimethalin induces Apoptotic cell death through activating ER stress-mediated mitochondrial dysfunction in human umbilical vein endothelial cells.
    Pendimethalin
  • HY-128553
    Antineoplaston A10
    		Inhibitor 98.54%
    Antineoplaston A10 is an antineoplaston that inhibits the growth of human hepatoma cells by inducing apoptosis. Antineoplaston A10 can be used in the study of liver cancer and breast cancer.
    Antineoplaston A10
  • HY-P1889
    Bim BH3, Peptide IV
    		99.35%
    Bim BH3, Peptide IV is a 26-residue peptide from BH3-only protein Bim, which belongs to the pro-apoptotic group of the Bcl-2 family of proteins.
    Bim BH3, Peptide IV
  • HY-12527
    Pyridoclax
    		Inhibitor 99.95%
    Pyridoclax is a potential Mcl-1 inhibitor.
    Pyridoclax
  • HY-15341
    BAM7
    		Activator 98.53%
    BAM7 is a direct and selective activator of proapoptotic BAX with an IC50 of 3.3 μM.
    BAM7
  • HY-P1562
    PUMA BH3
    		Activator 98.24%
    PUMA BH3 is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide, acts as a direct activator of Bak, with a Kd of 26 nM.
    PUMA BH3
  • HY-N1440
    Koumine
    		Activator 99.97%
    Koumine is an alkaloid separated from Gelsemium elegans, shows potent anti-tumor activity. Koumine up-regulates the Bax/Bcl-2 ratio and caspase-3 expression in human breast cancer cells. Koumine has anxiolytic, antistress, antipsoriatic, and analgesic activities, protects against the development of arthritis in Rheumatoid arthritis (RA) animal models.
    Koumine
  • HY-129700
    MCL-1/BCL-2-IN-2
    		Inhibitor 99.12%
    MCL-1/BCL-2-IN-2 (Compound 6) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor.
    MCL-1/BCL-2-IN-2
  • HY-16014
    A-385358
    		Inhibitor 98.19%
    A-385358 is a selective inhibitor of Bcl-XL with Kis of 0.80 and 67 nM for Bcl-XL and Bcl-2, respectively.
    A-385358
  • HY-110031
    BAI1 hydrochloride
    		Inhibitor 99.82%
    BAI1 hydrochloride is a selective apoptosis factor BAX allosteric inhibitors. BAI1 hydrochloride binds BAX and allosterically inhibits its activation. BAI1 hydrochloride has the potential to be used in the study of BAX dependent cell death-mediated diseases.
    BAI1 hydrochloride
  • HY-115532
    BCL6-IN-7
    		Inhibitor 99.79%
    BCL6-IN-7 is a potent BCL6−corepressor interaction inhibitor.
    BCL6-IN-7
  • HY-100502
    CID5721353
    		Inhibitor ≥98.0%
    CID5721353 is an inhibitor of BCL6 with an IC50 value of 212 μM, which corresponds to a Ki of 147 μM.
    CID5721353
Cat. No. Product Name / Synonyms Application Reactivity
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Download Bcl-2 Family Signaling Pathway Map.

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.

Bcl-2 Family Isoform Comparison

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