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-158551
    PROTAC BcI-2/BcI-xI Degrader-1
    		Degrader
    PROTAC BcI-2/BcI-xI Degrader-1 (15) is a PROTAC based BcI-2/BcI-xI degrader (Red: BcI-2/BcI-xI inhibitor (HY-158677), black: linker, Blue: E3 ligase ligand).
    PROTAC BcI-2/BcI-xI Degrader-1
  • HY-170929
    EMT inhibitor-3
    EMT inhibitor-3 (compound 11i) is a epithelial-mesenchymal transition (EMT) inhibitor. EMT inhibitor-3 inhibits neuroblastoma SK-N-SH cells with an IC50 of 2.5 μM. EMT inhibitor-3 inhibits SK-N-SH cell proliferation, migration, and invasion. EMT inhibitor-3 increases the Bax/Bcl-2 protein expression ratio, promotes Cytochrome C ( HY-125857) release from mitochondria, and activates caspases 9 and caspases 3, inducing mitochondria-mediated endogenous tumor cell Apoptosis. EMT inhibitor-3 is potential for cancer research.
    EMT inhibitor-3
  • HY-147928
    Apoptotic agent-2
    		Activator
    Apoptotic agent-2 (compound 14b) induces apoptosis by down-regulation of Bcl-2 and up-regulation of Bax and caspase-3. Apoptotic agent-2 exhibits anti-proliferative activities and can be used for cancer research.
    Apoptotic agent-2
  • HY-N3584R
    Paris saponin VII (Standard)
    		Inhibitor
    Paris saponin VII (Standard) is the analytical standard of Paris saponin VII. This product is intended for research and analytical applications. Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia.
    Paris saponin VII (Standard)
  • HY-P10993
    CT20p
    CT20p is an anticancer peptide based on the C hydrophobic terminus of Bax. CT20p has a unique cytotoxic effect independent of full-length Bax, and can act on mitochondria, leading to fusion-like aggregation and mitochondrial membrane hyperpolarization. CT20p can reduce α5β1 integrin levels and inhibit F-actin polymerization, thereby destroying the cytoskeleton and preventing cell attachment. CT20p can be used in the study of breast cancer.
    CT20p
  • HY-175037
    DNH28
    		Inhibitor
    DNH28 is a potent NF-κB and MAPK inhibitor with an IC50 of 0.93 μM against HepG2 cells. DNH28 promotes apoptosis by down-regulating the expression of Bcl-2, up-regulating the expression of BAX and Cleaved-caspase-3. DNH28 blocks the cell cycle and inhibits migration. DNH28 can be used for the study of hepatocellular carcinoma (HCC).
    DNH28
  • HY-15668
    ST09
    		Activator
    ST09 is an efficient and low toxicity curcumin derivative. ST09 significantly inhibits cell migration and downregulates the expression of MMP1, MMP2, and Vimentin. ST09 has strong cytotoxicity to breast cancer cells, such as MDA-MB-231, MCF7 and T47D cells. ST09 induces cell apoptosis by upregulating Bax and cleaved caspase-3/9. ST09 can be used in the research of cancer such as breast cancer.
    ST09
  • HY-145826
    Mcl-1 inhibitor 8
    		Inhibitor
    Mcl-1 inhibitor 8 is a MCL-1 inhibitor, example 228, extracted from patent WO2019222112.
    Mcl-1 inhibitor 8
  • HY-111467
    Mcl1-IN-4
    		Inhibitor
    Mcl1-IN-4 is an inhibitor of Mcl1 with an IC50 of 0.2 μM.
    Mcl1-IN-4
  • HY-149624
    Bcl-2-IN-14
    		Inhibitor
    Bcl-2-IN-14 (Compound 13c) is a BCL-2 inhibitor with an IC50 value of 0.471 μM. Bcl-2-IN-14 can be used in cancer research.
    Bcl-2-IN-14
  • HY-149009
    Bcl-2-IN-9
    		Inhibitor
    Bcl-2-IN-9 is a novel proapoptotic Bcl-2 inhibitor with IC50 value of 2.9 μM and low cytotoxic. Bcl-2-IN-9 mediates apoptosis by down-regulating expression of Bcl-2 in cancer cells and has a high selectivity against leukemia cells.
    Bcl-2-IN-9
  • HY-155406
    Estrogen receptor modulator 10
    		Inhibitor
    Estrogen receptor modulator 10 (compound G-5b) is an estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM). Estrogen receptor modulator 10 is developed based on the Fulvestrant (HY-13636) molecule and can rapidly degrade ER receptors through the proteasome pathway. Estrogen receptor modulator 10 can induce cell apoptosis and block cells in the G1/G0 phase and can be used in cancer research.
    Estrogen receptor modulator 10
  • HY-172877
    EGFR/BRAFV600E-IN-5
    		Inducer
    EGFR/BRAFV600E-IN-5 (Compound 7I) is a dual BRAFV600E/EGFR inhibitor with IC50 of 0.048 μM and 0.037 μM, respectively. EGFR/BRAFV600E-IN-5 has significant anti-melanoma activity with IC50 of 3.16 μM and 2.50 μM against MALME-3M and LOX-IMVI cell lines, respectively. EGFR/BRAFV600E-IN-5 exerts anti-tumor effects by inducing G1 arrest, inhibiting DNA synthesis, and activating the mitochondrial apoptosis pathway. EGFR/BRAFV600E-IN-5 can be used for melanoma research, especially for combined inhibition of BRAFV600E mutation and EGFR signaling pathway.
    EGFR/BRAFV600E-IN-5
  • HY-100866B
    F1324 acetate
    		Inhibitor
    F1324 acetate is a potent, high affinity peptidic inhibitor of B cell lymphoma 6 (BCL6), with an IC50 of 1 nM. F1324 acetate exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI.
    F1324 acetate
  • HY-112417
    Ki11502
    		Inhibitor 99.30%
    Ki11502 is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that selectively inhibits the activity of PDGF β/α receptors with IC50 values less than 10 nM. Ki11502 selectively inhibits PDGF β receptor phosphorylation, proliferation, and proteoglycan synthesis in human vascular smooth muscle cells. Ki11502 can induce Apoptosis) and exhibits profound antiproliferative effects on select subsets of leukemia, including those with Imatinib (HY-15463) resistant mutations. Ki11502 is highly suitable for studying the role of PDGF in vascular diseases, particularly the role of proteoglycans in atherosclerosis.
    Ki11502
  • HY-30219R
    D-(+)-Phenyllactic acid (Standard)
    		Inhibitor
    D-​(+)​-​Phenyllactic acid (Standard) is the analytical standard of D-​(+)​-​Phenyllactic acid. This product is intended for research and analytical applications. D-​(+)​-​Phenyllactic acid is an anti-bacterial agent, excreted by Geotrichum candidum, inhibits a range of Gram-positive from humans and foodstuffs and Gram-negative bacteria found in humans[1].
    D-(+)-Phenyllactic acid (Standard)
  • HY-175019
    VEGFR-2-IN-70
    		Agonist
    VEGFR-2-IN-70 is a potent VEGFR-2 inhibitor with an IC50 of 18.04 nM. VEGFR-2-IN-70 exhibits cytotoxicity against A549 and MCF-7 cancer cells with IC50 values of 0.43 μM and 3.8 μM, respectively. VEGFR-2-IN-70 induces G1 cell cycle arrest and apoptosis in lung cancer cells. VEGFR-2-IN-70 is useful in cancer research.
    VEGFR-2-IN-70
  • HY-172798
    XZ338
    		Degrader
    XZ338 is a highly selective degrader targeting BCL-XL. XZ338 does not degrade BCL-2. XZ338 inhibits MOLT-4 cells with a IC50 value of 3.7 nM. XZ338 has anti-proliferative activity. XZ338 can be used for anti-cancer study. (Target protein ligand: HY-19741; E3 ligase: HY-112078; linker: HY-172799; E3+liner: HY-172800).
    XZ338
  • HY-174404
    Topoisomerase II inhibitor 23
    		Inhibitor
    Topoisomerase II inhibitor 23 is a potent topoisomerase II inhibitor (IC50 = 0.94 μM). Topoisomerase II inhibitor 23 shows high selectivity and exceptional cytotoxic activity in MCF-7, HepG2, and HCT116 cells. Topoisomerase II inhibitor 23 induces cell cycle arrest at the G1 phase, leading to inhibition of cell proliferation. Topoisomerase II inhibitor 2 induces apoptosis by up-regulating the pro-apoptotic Bax level and down-regulating the anti-apoptotic Bcl-2 level.
    Topoisomerase II inhibitor 23
  • HY-170787
    TZEP7
    		Inhibitor
    TZEP7 is an EGFR kinase inhibitior in cancer cells. TZEP7 exhibits cytotoxic effects against cancer cell lines and induces apoptosis. TZEP7 demonstrates downregulation of antiapoptotic Bcl-2, upregulation of pro-apoptotic Bax, and increases caspase levels. TZEP7 is promising for research of anticancer agent.
    TZEP7
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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