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-10087S
    Navitoclax-d8
    		Inhibitor 99.71%
    Navitoclax-d8 is the deuterium labeled Navitoclax. Navitoclax (ABT-263) is a potent and orally active 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.
    Navitoclax-d<sub>8</sub>
  • HY-16695
    MIM1
    		Inhibitor ≥98.0%
    MIM-1 is an inhibitor of myeloid cell factor 1 (Mcl-1).
    MIM1
  • 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-108164
    Aspidin BB
    		Modulator 98.08%
    Aspidin BB is a phloroglucinol derivative, which can be isolated from the aerial part of Dryopteris championii. Aspidin BB has anticancer activity. Aspidin BB induces cell cycle arrest and apoptosis in human ovarian HO-8910 cells.
    Aspidin BB
  • HY-100741C
    (R,R)-S63845
    		Control 99.32%
    (R,R)-S63845 is the isomer of S63845 (HY-100741), and can be used as an experimental control. S63845 is a potent and selective myeloid cell leukemia 1 (MCL1) inhibitor with a Kd of 0.19 nM for human MCL1.
    (R,R)-S63845
  • HY-12908
    Bcl-xL antagonist 2
    		Antagonist 98.86%
    Bcl-xL antagonist 2 is a potent, selective, and orally active antagonist of BCL-XL with an IC50 and Ki of 0.091 μM and 65 nM, respectively. Bcl-xL antagonist 2 promotes the apoptosis of cancer cells. Bcl-xL antagonist 2 has the potential for the research of the chronic lymphocytic leukemia (CLL) and non-Hodgkin’s lymphoma (NHL).
    Bcl-xL antagonist 2
  • HY-N6573
    Bufarenogin
    		Activator 99.36%
    Bufarenogin induces intrinsic apoptosis via Bax and ANT cooperation.
    Bufarenogin
  • HY-132173
    GL0388
    		Activator 98.01%
    GL0388 is a Bax activator that results in Bax insertion into mitochondrial membrane. GL0388 shows antiproliferative activities against various cancer cells, with IC50s of 0.299-1.57 μM. GL0388 activates Bax and induce Bax-mediated apoptosis. GL0388 suppresses breast cancer xenograft tumor growth in vivo.
    GL0388
  • HY-128553
    Antineoplaston A10
    		Inhibitor 99.84%
    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-147187
    MNK8
    		Inhibitor 99.76%
    MNK8 is a potent STAT3 (signal transducer and activator of transcription 3) inhibitor. MNK8 inhibits STAT3 activation and reduced its DNA binding ability. MNK8 shows good growth inhibition against hepatocellular carcinoma (HCC) cells. MNK8 induces apoptosis in HCC cells. MNK8 reduces prosurvival proteins expression and migration/invasion of HCC cells.
    MNK8
  • HY-169266
    BRD-K56819078
    		Inhibitor 99.58%
    BRD-K56819078 is a Bcl-2 inhibitor that significantly reduces senescent cell load and senescence-related genes in the kidney mRNA expression. BRD-K56819078 exerts anti-aging effects by inhibiting apoptosis.
    BRD-K56819078
  • HY-N4238
    Dehydrocorydaline nitrate
    		Inhibitor 99.90%
    Dehydrocorydaline nitrate (13-Methylpalmatine nitrate) is an alkaloid. Dehydrocorydaline regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP. Dehydrocorydaline nitrate elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities.. Dehydrocorydaline nitrate shows strong anti-malarial effects (IC50 =38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain.
    Dehydrocorydaline nitrate
  • HY-131232
    Desmorpholinyl Navitoclax-NH-Me
    		Inhibitor 98.64%
    Desmorpholinyl Navitoclax-NH-Me is a Bcl-xL inhibitor. Desmorpholinyl Navitoclax-NH-Me and a CRBN ligand for the E3 ubiquitin ligase can be used in the synthesis of PROTAC BCL-XL degrader XZ739 (HY-133557).
    Desmorpholinyl Navitoclax-NH-Me
  • HY-N1157
    Thevetiaflavone
    		Modulator ≥98.0%
    Thevetiaflavone could upregulate the expression of Bcl-2 and downregulate that of Bax and caspase-3.
    Thevetiaflavone
  • HY-112591
    NSC260594
    		Inhibitor
    NSC260594 induces Apoptosis. NSC260594 binds the shallow groove of the Mcl-1 protein, and inhibits Mcl-1 expression through down-regulation of Wnt signaling proteins. NSC260594 can also recognize G9-G10-A11-G12 RNA tetraloop of HIV and prevent the binding of the Gag protein within the 5’-UTR. NSC260594 inhibits tumor growth, and can be used for research of Triple-negative breast cancers (TNBCs).
    NSC260594
  • HY-P5243
    Copper tripeptide-3
    		99.09%
    Copper tripeptide-3 (AHK-Cu) is a bioactive peptide with promotion of hair growth effect. Copper tripeptide-3 increases dermal cell proliferation and viability while increasing the deposition of collagen to renew the extracellular matrix. Copper tripeptide-3 stimulates the elongation of human hair follicles and proliferation of dermal papilla cells.
    Copper tripeptide-3
  • HY-122760
    Bax activator-1
    		Activator 98.45%
    Bax activator-1 (compound 106) is a Bax activator that induces Bax-dependent tumor cell apoptosis.
    Bax activator-1
  • HY-N0060BS
    (E)-Ferulic acid-d3
    		Activator ≥99.0%
    (E)-Ferulic acid-d3 is the deuterium labeled (E)-Ferulic acid. (E)-Ferulic acid is a isomer of Ferulic acid which is an aromatic compound, abundant in plant cell walls. (E)-Ferulic acid causes the phosphorylation of β-catenin, resulting in proteasomal degradation of β-catenin and increases the expression of pro-apoptotic factor Bax and decreases the expression of pro-survival factor survivin. (E)-Ferulic acid shows a potent ability to remove reactive oxygen species (ROS) and inhibits lipid peroxidation. (E)-Ferulic acid exerts both anti-proliferation and anti-migration effects in the human lung cancer cell line H1299.
    (E)-Ferulic acid-d<sub>3</sub>
  • HY-129700
    MCL-1/BCL-2-IN-2
    		Inhibitor 99.05%
    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-15531R
    Venetoclax (Standard)
    		Inhibitor
    Venetoclax (Standard) is the analytical standard of Venetoclax. This product is intended for research and analytical applications. Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy.
    Venetoclax (Standard)
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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