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-175589
    XSJ81
    		Inhibitor
    XSJ81 is an orally active anti-cancer agent. XSJ81 significantly inhibits the proliferation of ampullary carcinoma (AC) DPC-X3 cells with an IC50 of 0.655 μM. XSJ81 inhibits the colony formation, arrests cell cycle at the G2/M phase and inhibits the migration in DPC-X3 cells. XSJ81 induces DNA damage and apoptosis in DPC-X3 cells. XSJ81 demonstrates significant anti-tumor efficacy in mice bearing DPC-X3 xenografts. XSJ81 can be used for the study of ampullary carcinoma.
    XSJ81
  • HY-178380
    HDAC8-IN-14
    		Activator
    HDAC8-IN-14, a curcuminoid derivative, is a selective HDAC8 inhibitor with a Ki of 9 nM. HDAC8-IN-14 induces the production of reactive oxygen species (ROS), disrupts mitochondrial membrane potential, and promotes apoptosis. HDAC8-IN-14 can significantly promote the accumulation of cells in the sub-G0/G1 phase, consistent with apoptotic or necrotic cell death. HDAC8-IN-14 induces upregulation of cytochrome c, cleaved caspase-3, and the pro-apoptotic protein Bak while leaving the anti-apoptotic Bcl-2 levels unaltered. HDAC8-IN-14 can be used for the study of leukemia.
    HDAC8-IN-14
  • HY-RS01374
    BAX Human Pre-designed siRNA Set A
    		Inhibitor

    BAX Human Pre-designed siRNA Set A contains three designed siRNAs for BAX gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    BAX Human Pre-designed siRNA Set A
  • HY-124846
    MI-223
    		Modulator
    MI-223 is a Mcl-1 regulator (Kd = 160 nM). MI-223 binds to the BH1 domain, blocking Mcl-1-stimulated homologous recombination DNA repair, thus sensitizing cancer cells to DNA replication agents. MI-223 can be used in research on cancers such as lung cancer.
    MI-223
  • HY-121859
    RU28362
    		Activator
    RU28362 is a potent and selective glucocorticoid agonist. RU28362 increases the Bnip3 mRNA levels in neurons. RU28362 inhibits adrenocorticotrophic hormone (ACTH) and corticosterone secretion. RU28362 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    RU28362
  • HY-P1562A
    PUMA BH3 TFA
    		Activator
    PUMA BH3 TFA 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 TFA
  • HY-127130
    Spicamycin
    		Inhibitor
    Spicamycin, an adenine nucleoside antibiotic with antifungal and antitumor activities. Spicamycin is also a potent inducer of differentiation of myeloid leukemia cells. Spicamycin induces apoptosis in NB4 cells via down-regulation of Bcl-2 expression and modulation of PML protein.
    Spicamycin
  • HY-B0402R1
    Amantadine in Methanol (Standard)
    		Modulator
    Amantadine in Methanol (Standard) is the solution of Amantadine (Standard). This product is intended for research and analytical applications. Amantadine (1-Adamantanamine) is an orally avtive and potent antiviral agent with activity against influenza A viruses. Amantadine inhibits several ion channels such as NMDA and M2, and also inhibits Coronavirus ion channels. Amantadine also has anti-orthopoxvirus and anticancer activity. Amantadine can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research[4].
    Amantadine in Methanol (Standard)
  • HY-169431
    VEGFR-2/AKT-IN-2
    		Inhibitor
    VEGFR-2/AKT-IN-2 (Compound 5) is a VEGFR-2/AKT inhibitor (IC50: 0.061 μM for VEGFRin HepG2 cell). VEGFR-2/AKT-IN-2 reduces total and phosphorylated AKT as well as up-regulates BAX and Caspase-3 and down-regulates Bcl-2 in cells, thereby promoting Apoptosis. VEGFR-2/AKT-IN-2 causes cell cycle arrest in S phase. VEGFR-2/AKT-IN-2 inhibits the growth of human liver tumor cells.
    VEGFR-2/AKT-IN-2
  • HY-176740
    PROTAC Bcl-xL degrader-4
    		Degrader
    PROTAC Bcl-xL degrader-4 (Compound 2-38-III) is a Bcl-xL PROTAC degrader. PROTAC Bcl-xL degrader-4 has strong anti-tumor activity against HepG2 cells and HUVEC cells. PROTAC Bcl-xL degrader-4 induces cells apoptosis by decreasing mitochondrial membrane potential and activating the MAPK signaling pathway. PROTAC Bcl-xL degrader-4 significantly inhibits tumor growth in xenograft tumor mouse models. Pink: MAPK ligand (HY-176741); Blue: CRBN ligase ligand (HY-10984); Black: linker (HY-W017440)
    PROTAC Bcl-xL degrader-4
  • HY-136714
    Bcl-2-IN-3
    		Inhibitor
    Bcl-2-IN-3 (Compound 10) is a Bcl-2 inhibitor. Bcl-2-IN-3 can be used for the research of cancer.
    Bcl-2-IN-3
  • HY-N2897R
    Dihydrokaempferol (Standard)
    		Inhibitor
    Dihydrokaempferol (Standard) is the analytical standard of Dihydrokaempferol. This product is intended for research and analytical applications. 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 (Standard)
  • HY-W050044R
    L-Azetidine-2-carboxylic acid (Standard)
    		Activator
    L-Azetidine-2-carboxylic acid is a proline analog. L-Azetidine-2-carboxylic acid upregulates the lipid autophagy marker LC3-II via activation of the PERK pathway. L-Azetidine-2-carboxylic acid increases pro-apoptotic BAX protein. L-Azetidine-2-carboxylic acid induces ATF6 cleavage and upregulates phosphorylated eIF2α levels. L-Azetidine-2-carboxylic acid induces ER stress, inducing protein misfolding and aggregation. L-Azetidine-2-carboxylic acid shows teratogenic, pro-inflammatory and pro-apoptotic effects.
    L-Azetidine-2-carboxylic acid (Standard)
  • HY-115529
    (-)BI97D6
    (-)BI97D6 is a broad-spectrum inhibitor of the Bcl-2 protein family, inhibiting Mcl-1, Bcl-2, Bcl-xL and Bcl-1 with IC50 values ​​of 0.025, 0.031, 0.076 and 0.122 μM, respectively. (-)BI97D6 stimulates cell death through the Bak and Bax mediated mitochondrial apoptosis pathway. In addition, (-)BI97D6 inhibits Mcl-1 and can effectively induce apoptosis in acute myeloid leukemia (AML) cells.
    (-)BI97D6
  • HY-171031
    TFGF-18
    TFGF-18 is a GSK-3β inhibitor (IC50: 0.59 μM). TFGF-18 inhibits LPS-induced microglia activation and proinflammatory mediators release via inhibiting GSK-3β and downstream p65/NF-κB signaling. TFGF-18 inhibits neuronal apoptosis and oxidative stress, inhibits expressions of Bax, caspase3 and cleaved-caspase3 and increases the expression of Bcl-2. TFGF-18 has neuroprotection effect, inhibit neuroinflammation and attenuates cognitive impairment.
    TFGF-18
  • HY-16232R
    Glufosfamide (Standard)
    		Inhibitor
    Glufosfamide (Standard) is the analytical standard of Glufosfamide. This product is intended for research and analytical applications. Glufosfamide is a glucose-conjugated alkylating cytotoxic agent and a derivative of Ifosfamide (HY-17419). Glufosfamide induces apoptosis frequency and increase the expression of caspase-9 and caspase-3 in cancer cells. Glufosfamide shows great anti-tumor activity in MiaPaCa-2-RFP mouse model. Glufosfamide can be used for the study of hepatocellular carcinoma, prostate cancer and pancreatic carcinoma.
    Glufosfamide (Standard)
  • HY-15613R
    Maritoclax (Standard)
    		Inhibitor
    Maritoclax (Standard) is the analytical standard of Maritoclax. This product is intended for research and analytical applications. Maritoclax (Marinopyrrole A) is a novel and specific Mcl-1 inhibitor with an IC50 value of 10.1 μM, and shows >8 fold selectivity than BCL-xl (IC50 > 80 μM).
    Maritoclax (Standard)
  • HY-101083A
    (Rac)-BDA-366
    		Inhibitor
    (Rac)-BDA-366 (example 2) is the despinner of BDA-366 (HY-101083). BDA-366 is a potent Bcl-2 antagonist (Ki=3.3 nM), binding Bcl-2-BH4 domain with high affinity and selectivity. BDA-366 induces conformational change in Bcl-2 that abrogates its antiapoptotic function, converting it from a survival molecule to a cell death inducer. BDA-366 suppresses growth of lung cancer cells.
    (Rac)-BDA-366
  • HY-12011A
    (Rac)-HA14-1
    		Inhibitor
    (Rac)-HA14-1 is the racemic form of HA14-1 (HY-12011). HA14-1 is a Bcl-2/Bcl-xL antagonist with an IC50 of approximately 9 μM against Bcl-2.
    (Rac)-HA14-1
  • HY-119682
    Bax agonist 1
    Bax agonist 1 (compound SMBA2) is a Bax agonist (Ki=57.2 nM). Bax agonist 1 induces Bax conformational changes by blocking S184 phosphorylation, promoting Bax insertion into the mitochondrial membrane and forming Bax oligomers, which induce cytochrome c release and apoptosis in malignant cancer cells expressing Bax. Bax agonist 1 can be used in lung cancer research.
    Bax agonist 1
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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