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-B1971
    Deltamethrin
    		99.93%
    Deltamethrin (Decamethrin) is an orally active synthetic pyrethroid insecticide. Deltamethrin induces oxidative stress and results in inflammation and apoptosis via inhibiting Nrf2/HO-1 pathway. Deltamethrin has an anticancer effect by inducing apoptosis. Deltamethrin can be used extensively in pest control.
    Deltamethrin
  • HY-18705
    Azoramide
    		Inhibitor 99.57%
    Azoramide is a potent, orally active small-molecule modulator of the unfolded protein response (UPR). Azoramide improves ER protein folding and elevates ER chaperone capacity, which together protects cells against ER stress. Azoramide alleviates PLA2G6 mutant-induced ER stress through modulating unfolded protein response, and enhances the CERB signaling to rescue mitochondrial function, thereby preventing apoptosis of DA neurons. Azoramide has antidiabetic activity.
    Azoramide
  • HY-N0279
    Cardamonin
    		Inhibitor 99.80%
    Cardamonin can be found from cardamom, and can target various signaling molecules, transcriptional factors, cytokines and enzymes. Cardamonin can inhibit mTOR, NF-κB, Akt, STAT3, Wnt/β-catenin and COX-2. Cardamonin shows anticancer, anti-inflammatory, antimicrobial and antidiabetic activities.
    Cardamonin
  • HY-129960
    L-Selenocystine
    		98.0%
    L-Selenocystine is a selenium-containing amino acid. L-Selenocystine has redox properties. L-Selenocystine is cytotoxic to various tumor cells and can induce the production of ROS and apoptosis. L-Selenocystine can block the Nrf2 and autophagy pathways. L-Selenocystine has anti-tumor activity.
    L-Selenocystine
  • HY-129179
    Lisaftoclax
    		Inhibitor 99.78%
    Lisaftoclax (compound 6) is a dual Bcl-2 and Bcl-xl inhibitor with anti-tumor activity, extracted from patent WO2018027097A1. Lisaftoclax exhibits IC50 values of 2 nM and 5.9 nM for Bcl-2 and Bcl-xl, respectively.
    Lisaftoclax
  • HY-126741
    Azadirachtin
    		Inhibitor 99.06%
    Azadirachtin is an oral active triterpenoid compound with anticancer, antimalarial, anti-inflammatory, and insecticidal activities. Azadirachtin induces cell apoptosis through the mitochondrial pathway (by inhibiting Bcl-2/Bax ratio or activating Apaf-1 and caspase-3) or through death receptors (by inhibiting TNFR activation). Additionally, Azadirachtin exerts its anti-inflammatory effects by inhibiting NF-кB signaling pathway activation, and it exhibits insecticidal activity by inducing apoptosis in insect cells.
    Azadirachtin
  • HY-149672
    ABBV-467
    		Inhibitor 99.78%
    ABBV-467 is a selective MCL-1 inhibitor (Ki: <0.01 nM). ABBV-467 induces apoptosis. ABBV-467 induces cancer cell death and inhibits tumor growth in models of hematological malignancies, such as multiple myeloma.
    ABBV-467
  • HY-120079
    MSN-125
    		Inhibitor 99.00%
    MSN-125 is a potent Bax and Bak oligomerization inhibitor. MSN-125 prevents mitochondrial outer membrane permeabilization (MOMP) with an IC50 of 4 μM. MSN-125 potently inhibits Bax/Bak-mediated apoptosis in HCT-116, BMK Cells, and primary cortical neurons, protects primary neurons against glutamate excitotoxicity.
    MSN-125
  • HY-113427
    trans-Vaccenic acid
    		Inhibitor 98.0%
    trans-Vaccenic acid is a naturally occurring trans fatty acid (TFA). trans-Vaccenic acid inhibits nasopharyngeal carcinoma (NPC) cell growth and induces apoptosis through the inhibition of Bad/Akt phosphorylation. trans-Vaccenic acid is a precursor for the synthesis of saturated fatty acid in the rumen and of conjugated Linoleic acid (CLA) at the tissue level. trans-Vaccenic acid exerts hypolipidemic effects in a rat model of obesity.
    trans-Vaccenic acid
  • HY-W250122
    Glutamic acid sodium salt
    		Activator 99.92%
    Glutamic acid sodium salt (Monosodium glutamate) is an orally active food flavor enhancer. Glutamic acid sodium salt causes ROS generation, mitochondrial dysfunction, and Apoptosis. Glutamic acid sodium salt upregulates CHOP, Grp78, and Bcl-2. Glutamic acid sodium salt impairs cognition, induces depressive-like behavior, induces hyperalgesia, and induces obesity and insulin resistance. Glutamic acid sodium salt can be used to study neurotoxicity (e.g., brain damage, cognitive impairment), metabolic disorders (e.g., obesity, insulin resistance), hepatotoxicity, and renal toxicity, as well as pain-related disorders.
    Glutamic acid sodium salt
  • HY-147081A
    AS 1411 sodium
    		Inhibitor 99.52%
    AS 1411 (AGRO-100) sodium is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 sodium inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 sodium reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. S 1411 sodium works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. S 1411 sodium-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity
    AS 1411 sodium
  • HY-N2897
    Dihydrokaempferol
    		Inhibitor 99.92%
    Dihydrokaempferol is isolated from Bauhinia championii (Benth). Dihydrokaempferol induces apoptosis and inhibits Bcl-2 and Bcl-xL expression. Dihydrokaempferol is a good candidate for new antiarthritic agents.
    Dihydrokaempferol
  • HY-13755A
    (R)-Sulforaphane
    		Inhibitor 99.95%
    (R)-Sulforaphane (L-Sulforaphane) is a orally active, potent inducer of the Keap1/Nrf2/ARE pathway, exhibiting antioxidant and anticancer activities. (R)-Sulforaphane primarily functions by upregulating phase II detoxifying enzymes in cells, aiding in the removal of carcinogens and combating oxidative stress. (R)-Sulforaphane is capable of modulating gene expression, influencing various signaling pathways, including Nrf2, NF-κB, and AP-1. (R)-Sulforaphane can be used in studies of tumor biology, antioxidant defense mechanisms, as well as inflammation and immune responses.
    (R)-Sulforaphane
  • HY-B0402A
    Amantadine hydrochloride
    		Modulator 98.0%
    Amantadine (1-Adamantanamine) hydrochloride is an orally avtive and potent antiviral agent with activity against influenza A viruses. Amantadine hydrochloride inhibits several ion channels such as NMDA and M2, and also inhibits Coronavirus ion channels. Amantadine hydrochloride also has anti-orthopoxvirus and anticancer activity. Amantadine hydrochloride can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research.
    Amantadine hydrochloride
  • HY-W250116
    Co(III) protoporphyrin IX chloride
    		Inducer
    Co(III) protoporphyrin IX chloride (Protoporphyrin IX cobaltic chloride) is an inducer of HO-1. Co(III) protoporphyrin IX chloride has activities such as anti-inflammation and antibacterial properties. Co(III) protoporphyrin IX chloride can also be used in the research of ischemia-reperfusion injury models.
    Co(III) protoporphyrin IX chloride
  • HY-12468
    A-1210477
    		Inhibitor 99.86%
    A-1210477 is a potent and selective inhibitor of MCL-1 with a Ki of 0.45 nM. A-1210477 specifically binds MCL-1 and promotes apoptosis of cancer cells in an MCL-1-dependent manner.
    A-1210477
  • HY-P99244
    Fezakinumab
    		Modulator 99.9%
    Fezakinumab (ILV 094) is an anti-IL-22 monoclonal antibody. Fezakinumab inhibits IL-22 signal transduction, and regulates the JAK1/STAT3 pathway as well as apoptotic proteins. Fezakinumab alleviates airway remodeling, alveolar enlargement and inflammatory cell infiltration in lung tissues. Fezakinumab reduces the levels of neutrophils, lymphocytes, eosinophils and macrophages in lung tissues. Fezakinumab can be used in the research of chronic obstructive pulmonary disease and skin diseases.
    Fezakinumab
  • HY-15607A
    WEHI-539 hydrochloride
    		Inhibitor 99.72%
    WEHI-539 hydrochloride is a selective inhibitor of Bcl-XL with an IC50 of 1.1 nM.
    WEHI-539 hydrochloride
  • HY-109185
    Pelcitoclax
    		Inhibitor 99.70%
    Pelcitoclax (APG-1252) is a potent Bcl-2/Bcl-xl inhibitor with antineoplastic and pro-apoptotic effects.
    Pelcitoclax
  • HY-B0766
    Bicyclol
    		99.91%
    Bicyclol (SY801) is an orally active derivative of the traditional Chinese medicine Schisandra chinensis, which has antiviral, anti-inflammatory, immunomodulatory, antioxidant, anti-steatosis, anti-fibrotic and anti-tumor activities. Bicyclol regulates the expression of heat shock proteins and plays an anti-apoptosis role in hepatocytes. Bicyclol reduces the activation of NF-κB and the levels of inflammatory factors in hepatocytes infected with hepatitis C virus (HCV) by inhibiting the activation of the ROS-MAPK-NF-κB pathway, and prevents ferroptosis in acute liver injury. Bicyclol can change the expression of Mdr-1, GSH/GST and Bcl-2, increase the intracellular concentration of anticancer drugs, and sensitize drug-resistant cells to anticancer drugs. Bicyclol inhibits the proliferation of human malignant hepatoma cells by regulating the PI3K/AKT pathway and the Ras/Raf/MEK/ERK pathway. Bicyclol can be used in the study of chronic hepatitis, acute liver injury, nonalcoholic fatty liver disease, liver fibrosis and hepatocellular carcinoma.
    Bicyclol
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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