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-101310
    SYM 2081
    		Activator 98.0%
    SYM 2081 is a kainate receptor agonist. SYM 2081 is a substrate of EAAT1 (Km of 54 μM). SYM 2081 inhibits EAAT2-mediated glutamate transport (Kb is 3.4 μM in Xenopus oocytes), modulates Apoptotic signaling pathways (increases Bcl-2 and decreases Bax/caspase-3 expression). SYM 2081 exhibits neuroprotective activity. SYM 2081 can be used in the study of hypoxic-ischemic brain damage and inflammatory or neuropathic pain.
    SYM 2081
  • HY-111237
    Butyrolactone I
    		Inhibitor 99.80%
    Butyrolactone I is an orally active and ATP-competitive inhibitor of CDK1. Butyrolactone I inhibits NF-κB, cdc2 kinase, Bax, ROS production, modulates the PERK/CHOP. Butyrolactone I mitigates heat-stress-induced Apoptosis. Butyrolactone I shows anti-inflammatory and intestinal protective activity. Butyrolactone I has antitumor effects against non-small cell lung, small cell lung, prostate cancer and leukemia. Butyrolactone I can be used in NASH research.
    Butyrolactone I
  • HY-15464D
    (S)-Gossypol (acetic acid)
    		Inhibitor 98.46%
    (S)-Gossypol is the isomer of a natural product Gossypol. (S)-Gossypol binds to the BH3-binding groove of Bcl-xL and Bcl-2 proteins with high affinity.
    (S)-Gossypol (acetic acid)
  • HY-N3031
    Grosvenorine
    		99.64%
    Grosvenorine is an orally active flavonoid glycoside found in S. grosvenorii. Grosvenorine exhibits antibacterial, antioxidant and antiinflammation activities. Grosvenorine can induce apoptosis and increases anti-apoptotic Bcl-2 protein expression and reduces pro-apoptotic P53 protein expression in gastric tissues. Grosvenorine enhances mucin/glycoprotein secretion, regulates gastric pH, and reduces gastric lesion incidence.Grosvenorine increases glutathione peroxidase, catalase, and SOD levels, reduces lipid peroxidation (MDA), and lowers TNF-α and IL-6 levels. Grosvenorine can be used for the researches of bacterial infection and Gastric ulcer.
    Grosvenorine
  • HY-133557
    XZ739
    		Inhibitor 99.08%
    XZ739, a Cereblon-dependent PROTAC BCL-XL (Bcl-2 family member) degrader with a DC50 value of 2.5 nM in MOLT-4 cells after 16 h treatment. XZ739 also induces cell death through caspase-mediated apoptosis.
    XZ739
  • HY-169266
    BRD-K56819078
    		Inhibitor 99.93%
    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-B2046
    Simazine
    		Inhibitor 99.44%
    Simazine is a triazine herbicide. Simazine is widely used in agriculture, potted plant and tree production. In addition, Simazine can induce the apoptosis of immune cells in the spleen of mice and inhibit the proliferation of B cells and T cells in mice.
    Simazine
  • HY-174876
    PZ671
    		Degrader 98.70%
    PZ671 is a potent Bcl-xL PROTAC degrader with an IC50 of 1.3 nM (MOLT-4 cells) and a DC50 of 0.9 nM (Bcl-xL). PZ671 induces apoptosis in MOLT-4 cells. PZ671 effectively inhibits tumor growth and rapidly reverses transient platelet counts reduction in MOLT-4 xenograft mice. PZ671 can be used for the research of cancer, such as small cell lung cancer (SCLC). (Structure Note: Pink: Bcl-xL ligand (HY-174878); Blue: CRBN Ligand (HY-138793); Black: linker; E3-linker (HY-174879))
    PZ671
  • 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-N0566
    23-Hydroxybetulinic acid
    		99.44%
    23-Hydroxybetulinic acid (Anemosapogenin) is an orally active triterpenoid with broad-spectrum anticancer activity. 23-Hydroxybetulinic acid reduces the levels of Bcl-2 and survivin, elevates the level of Bax, promotes the cleavage/activation of caspase-3 and caspase-9, and induces apoptosis via the endogenous mitochondrial pathway involving cytochrome C release and mitochondrial membrane potential disruption. 23-Hydroxybetulinic acid arrests the cell cycle at S and G1 phases, inhibits cancer cell proliferation, blocks the MAPK signaling pathway, regulates MMP2, and induces autophagic apoptosis by upregulating beclin-1. 23-Hydroxybetulinic acid inhibits the activity and efflux function of P-gp, increases the intracellular accumulation of chemotherapeutic drugs, and synergistically enhances cytotoxicity with Doxorubicin (HY-15142). 23-Hydroxybetulinic acid inhibits the phosphorylation and nuclear translocation of STAT6, blocks M2 macrophage polarization, and reduces M2 macrophage-mediated apoptosis resistance of colon cancer cells. 23-Hydroxybetulinic acid can be used in related studies on chronic myeloid leukemia, hepatocellular carcinoma, sarcoma 180, multidrug-resistant breast cancer, leukemia, Doxorubicin-induced cardiotoxicity, and colorectal cancer.
    23-Hydroxybetulinic acid
  • 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-157176
    BAX-IN-1
    		Inhibitor 98.05%
    BAX-IN-1 is a potential, selective inhibitor of Bcl-2-associated X protein (BAX).
    BAX-IN-1
  • HY-N0905
    Ginsenoside Rh4
    		Activator 99.28%
    Ginsenoside Rh4 is a rare saponin obtained from Panax notoginseng. Ginsenoside Rh4 activates Bax, caspase 3, caspase 8, and caspase 9. Ginsenoside Rh4 also induces autophagy.
    Ginsenoside Rh4
  • HY-139309
    PROTAC Bcl-xL degrader-2
    		Inhibitor 98.23%
    PROTAC Bcl-xL degrader-2 is a potent Bcl-xL (Bcl-2 family member) degrader based on von Hippel-Lindau ligand, with an IC50 of 0.6 nM.
    PROTAC Bcl-xL degrader-2
  • HY-15464A
    (R)-(-)-Gossypol acetic acid
    		Inhibitor 98.93%
    (R)-(-)-Gossypol acetic acid (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.
    (R)-(-)-Gossypol acetic acid
  • HY-120882
    BM-1197
    		Inhibitor 99.48%
    BM-1197 (UBX1967) is a potent and selective inhibitor of dual Bcl-2/Bcl-xL, with IC50s of 3.5 nM and 5.2 nM for Bcl-2 and Bcl-xL, respectively. BM-1197 exhibits antitumor effects both in vitro and in vivo.
    BM-1197
  • HY-W013105
    Sodium glycocholate hydrate, 98%
    		Modulator 99.91%
    Sodium glycocholate hydrate, 98% is a bile acid derivative. Sodium glycocholate hydrate, 98% downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Sodium glycocholate hydrate, 98% inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Sodium glycocholate hydrate, 98% modulates related bile acid receptor signaling. Sodium glycocholate hydrate, 98% suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Sodium glycocholate hydrate, 98% can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).
    Sodium glycocholate hydrate, 98%
  • HY-107835
    Flumethrin
    		99.29%
    Flumethrin (FCR 2769) is a pyrethroid insecticide and acaricide. Flumethrin targets voltage-gated sodium channels and estrogen receptor α (ERα). Flumethrin induces cytotoxicity, apoptosis, genotoxicity and DNA damage in breast cancer cells by regulating the expression of BCL2, BAX, TP53 and P21 genes. Flumethrin is applicable to relevant studies on ectoparasite infections (tick and flea burdens) in dogs and cats, as well as breast cancer.
    Flumethrin
  • HY-N1983
    Caudatin
    		99.95%
    Caudatin is an orally active and brain-penetrant C-21 steroidal found in Cynanchum bungei decne with a variety of biological activities. Caudatin can inhibit cell proliferation, migration, invasion, cause cell phase arrest, induce apoptosis, autophagy, ROS prodution and loss of mitochondrial membrane potential. Caudatin activates PARP, caspase-3, -7, -9, upregulates pro-apoptotic Bad and Bax and downregulates anti-apoptotic Bcl-2 and Bcl-XL. Caudatin suppresses VEGF, FAK phosphorylation, upregulates p21, p27, DR5 protein expression, activates the p38 MAPK, JNK and PPARα/TFEB-mediated autophagy-lysosomal signaling pathways. Caudatin can be used for the research of cancer, inflammation and neurological disease, such as glioma and Alzheimer's disease.
    Caudatin
  • HY-172209
    PPIA-IN-1
    		Inhibitor
    PPIA-IN-1 is a PPIA inhibitor with a Kd value of 0.52 μM. PPIA-IN-1 inhibits the PPIA/MAPK signaling pathway to exert antiproliferative activity. PPIA-IN-1 induces G0/G1 cell cycle arrest in cancer cells. PPIA-IN-1 upregulates the expression of Bax and caspase-3, downregulates Bcl-2 expression, and induces apoptosis in cancer cells. PPIA-IN-1 induces increased ROS levels, DNA damage, endoplasmic reticulum stress, and mitochondrial dysfunction in cancer cells. PPIA-IN-1 exhibits antitumor activity in a mouse colon cancer xenograft model. PPIA-IN-1 can be used for the research of colorectal cancer.
    PPIA-IN-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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