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-P5342
    Hrk BH3
    Hrk BH3 is a biological active peptide. (BH3 domain of Hrk)
    Hrk BH3
  • HY-174469
    PROTAC PI3K/110β degrader-2
    		Inhibitor
    PROTAC PI3K/110β degrader-2 is a selective PI3K/p110β PROTAC degrader. PROTAC PI3K/110β degrader-2 can significantly degrade 110β protein and inhibit the expression of P-glycoprotein. PROTAC PI3K/110β degrader-2 can increase the level of reactive oxygen species (ROS). PROTAC PI3K/110β degrader-2 exerts anti-tumor effects by activating the endoplasmic reticulum stress (ERS)-mediated mitochondrial apoptosis pathway and inhibiting the AKT/Bcl-2 signaling pathway. PROTAC PI3K/110β degrader-2 can be used for research on cancer. (Pink: PI3K/110β Ligand (HY-75124); Blue: VHL Ligand (HY-125845); Black: Linker (HY-W002042)).
    PROTAC PI3K/110β degrader-2
  • HY-12048R
    Chelerythrine chloride (Standard)
    		Inhibitor
    Chelerythrine (chloride) (Standard) is the analytical standard of Chelerythrine (chloride). This product is intended for research and analytical applications. Chelerythrine chloride is a potent, cell-permeable inhibitor of protein kinase C, with an IC50 of 660 nM. Chelerythrine chloride inhibits the Bcl-XL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from Bcl-XL. Chelerythrine chloride induces apoptosis and autophagy.
    Chelerythrine chloride (Standard)
  • HY-13407R
    Gossypol (Standard)
    		Antagonist
    Gossypol (Standard) is the analytical standard of Gossypol. This product is intended for research and analytical applications. Gossypol binds to Bcl-xL protein and Bcl-2 protein with Kis of 0.5-0.6 μM and 0.2-0.3 mM, respectively.
    Gossypol (Standard)
  • HY-120275
    CYD-2-11
    		Agonist
    CYD-2-11 is a selective Bax agonist with a Ki value of 34.1 nM. CYD-2-11 induces cell apoptosis and shows antiproliferative activity to breast cancer MDA-MB-231 and MCF-7 cell lines with IC50 values of 3.22 and 3.81 μM, respectively. CYD-2-11 suppresses tumor growth in MDA-MB-231 tumor models. CYD-2-11 can be used for the research of breast and lung cancer.
    CYD-2-11
  • HY-149625
    Bcl-2-IN-15
    		Inhibitor
    Bcl-2-IN-15 (Compound 13d)) is a Bcl-2 inhibitor (IC50: 363 nM). Bcl-2-IN-15 inhibits the proliferation ofNCI leukemia cancer cell line.
    Bcl-2-IN-15
  • HY-P10832
    ATWLPPRAANLLMAAS
    ATWLPPRAANLLMAAS is a chimeric peptide with anti-angiogenic and potent anti-tumor effects. ATWLPPRAANLLMAAS can inhibit the proliferation, viability, migration, and invasion of human hepatocellular carcinoma cells, and induce apoptosis..
    ATWLPPRAANLLMAAS
  • HY-163309
    Bcl-2-IN-19
    		Inhibitor
    Bcl-2-IN-19 (compound 27) is a potent Bcl-2 inhibitor for targeting breast cancer.
    Bcl-2-IN-19
  • 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-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-172262
    WEHI-3773
    		Inhibitor
    WEHI-3773 is an inhibitor of the interaction between VDAC2 and BAK or BAX. WEHI-3773 inhibits BAX-mediated Apoptosis by blocking the VDAC2-mediated recruitment of BAX to mitochondria. Conversely, WEHI-3773 promotes BAK-mediated Apoptosis by limiting the inhibitory sequestration of BAK by VDAC2. WEHI-3773 is promising for research in the field of anti-cancer .
    WEHI-3773
  • 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-N13869
    Asperlin
    		Inhibitor
    Asperlin is an orally active marine-derived antibiotic with antifungal, anticancer, anti-inflammatory and anti-atherosclerotic activities. Asperlin induces apoptosis. Asperlin increases reactive oxygen species (ROS)- and DNA damage-associated G2/M phase arrest and ATM phosphorylation. Asperlin is effective in preventing HFD-induced obesity and modulating gut microbiota.
    Asperlin
  • 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-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
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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