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-129701
    MCL-1/BCL-2-IN-3
    		Inhibitor 98.93%
    MCL-1/BCL-2-IN-3 (Compound 2) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor with IC50s of 5.95 and 4.78 μM, respectively.
    MCL-1/BCL-2-IN-3
  • HY-160108
    Bcl-2-IN-17
    		Inhibitor
    Bcl-2-IN-17 is a Bcl2 inhibitor and can be used for the research of diseases associated with Bcl anti-apoptotic protein.
    Bcl-2-IN-17
  • HY-161242
    CBI1
    		Inhibitor
    CBI1 is a covalent BAX inhibitor. CBI1 selectively derivatizes BAX at C126 and inhibits BAX activation by triggering ligands or point mutagenesis. CBI1 blocks t-2-hex lipidation and oligomerization of BAX. CBI1 inhibits BAX activation induced by BH3 ligands, F116A mutagenesis or t-2-hex.
    CBI1
  • HY-146548
    Anticancer agent 43
    		Inducer 98.58%
    Anticancer Agent 43 is a potent anticancer agent. Anticancer Agent 43 induces apoptosis by caspase 3, PARP1, and Bax dependent mechanisms. Anticancer Agent 43 induces DNA damage.
    Anticancer agent 43
  • HY-P2468
    BAD (103-127) (human)
    		Inhibitor 98.80%
    BAD (103-127) (human), the 25-mer Bad peptide, is derived from the BH3 domain of BAD, can antagonize the function of Bcl-xL. BAD (103-127) (human) is reported to have almost 800-fold higher affinity for Bcl-XL than the 16-mer peptide.
    BAD (103-127) (human)
  • HY-P5325A
    Bid BH3 (80-99) acetate
    		98.13%
    Bid BH3 (80-99) (acetate) is a biological active peptide. (BID is a pro-apoptotic member of the 'BH3-only' (BOPS) subset of the BCL-2 family of proteins that constitute a critical control point in apoptosis. Bid is the first of the BOPs reported to bind and activate Bcl-2, Bax, and Bak. Bid serves as a death-inducing ligand that moves from the cytosol to the mitochondrial membrane to inactivate Bcl-2 or to activate Bax.Pyroglutamyl (pGlu) peptides may spontaneously form when either Glutamine (Q) or Glutamic acid (E) is located at the sequence N-terminus. The conversion of Q or E to pGlu is a natural occurrence and in general it is believed that the hydrophobic γ-lactam ring of pGlu may play a role in peptide stability against gastrointestinal proteases. Pyroglutamyl peptides are therefore considered a normal subset of such peptides and are included as part of the peptide purity during HPLC analysis.)
    Bid BH3 (80-99) acetate
  • HY-B0464S1
    Hydralazine-d5 hydrochloride
    Hydralazine-d5 (hydrochloride) is deuterium-labeled Hydralazine (hydrochloride) (HY-B0464).
    Hydralazine-d<sub>5</sub> hydrochloride
  • HY-115718A
    PZ703b TFA
    		Degrader 98.62%
    PZ703b TFA is a Bcl-xl PROTAC degradation agent that induces apoptosis and inhibits cancer cell proliferation for bladder cancer research.
    PZ703b TFA
  • HY-161659
    Apoptosis inducer 19
    		Modulator 98.31%
    Apoptosis inducer 19 (Compound 7g) is an Apoptosis inducer. Apoptosis inducer 19 elevates expression of pro-apoptotic proteins (Bax and caspase-3) and downregulates anti-apoptotic protein (Bcl-2). Apoptosis inducer 19 upregulates cellular reactive oxygen species (ROS) levels and disrupts mitochondrial membrane potential (MMP). Apoptosis inducer 19 can be used for triple-negative breast cancer (TNBC) research.
    Apoptosis inducer 19
  • HY-174873
    AF151
    		Inhibitor
    AF151 is a METTL3 PROTAC degrader with the DC50 of 0.43 μM in MOLM-13 cells. AF151 inhibits cell growth by significantly degrading METTL3 protein and reducing m6A levels. AF151 can induce cell apoptosis and reduce the level of Bcl-2 protein. AF151 can be used for research on cancer such as acute myeloid leukemia (AML). (Pink: METTL3 Ligand (HY-174874); Blue: VHL Ligand (HY-125845); Black: Linker; VHL Ligand+Linker (HY-174875)).
    AF151
  • HY-177102
    Mesutoclax
    		Inhibitor
    Mesutoclax (ICP-248) (Compound 5) is a selective BCL-2 inhibitor with an IC50 of 1.54 nM. Mesutoclax has weak activity against BCL-XL (IC50: ＞1000 nM). Mesutoclax can inhibit the activity of RS4;11 cells with an IC50 of 2.75 nM. Mesutoclax can be used in the study of cancer.
    Mesutoclax
  • HY-N2693
    6,8-Diprenylorobol
    		Modulator 98.40%
    6,8-Diprenylorobol, a prenylated isoflavone, is a nature product that could be isolated from the leaves of Cudrania tricuspidata. 6,8-Diprenylorobol antiproliferative effect and induces apoptosis through activation of p53 and generation of ROS.
    6,8-Diprenylorobol
  • HY-RS01421
    BCL2L1 Human Pre-designed siRNA Set A
    		Inhibitor

    BCL2L1 Human Pre-designed siRNA Set A contains three designed siRNAs for BCL2L1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    BCL2L1 Human Pre-designed siRNA Set A
  • HY-16669
    Mcl1-IN-1
    		Inhibitor 98.02%
    Mcl1-IN-1 is an inhibitor of myeloid cell factor 1 (Mcl-1) (IC50=2.4 µM).
    Mcl1-IN-1
  • HY-152169
    BIHC
    		Inhibitor ≥98.0%
    BIHC is a TNF blocker with anti-inflammatory activity. BIHC can significantly inhibit the proliferation of hepatocellular carcinoma (HCC) cells and exhibits potent cytotoxicity against the HepG2 cell line, capable of inducing cell apoptosis , while demonstrating relatively low toxicity towards normal hepatocytes. Additionally, BIHC can be used for research on inflammatory bowel disease (IBD).
    BIHC
  • HY-B0621R
    Triclabendazole (Standard)
    Triclabendazole (Standard) is the analytical standard of Triclabendazole. This product is intended for research and analytical applications. Triclabendazole is an orally active parasite inhibitor. Triclabendazole has anti-Leishmania activity and induces gasdermin E (GSDME)-dependent pyroptosis by caspase-3 activation. Triclabendazole can be used for the research of fasciola hepatica.
    Triclabendazole (Standard)
  • HY-10087R
    Navitoclax (Standard)
    		Inhibitor
    Navitoclax (Standard) is the analytical standard of Navitoclax. This product is intended for research and analytical applications. Navitoclax (ABT-263) is a potent and orally active Bcl-2 family protein inhibitor that binds to multiple anti-apoptotic Bcl-2 family proteins, such as Bcl-xL, Bcl-2 and Bcl-w, with a Ki of less than 1 nM.
    Navitoclax (Standard)
  • HY-175208
    MST3-IN-1
    		Inhibitor
    MST3-IN-1 is a selective and orally active MST3 inhibitor, with an IC50 of 122.4 nM. MST3-IN-1 shows antiproliferative activity against HepG2 cell. MST3-IN-1 effectively induces apoptosis in HepG2 cells, and halts the cell cycle at the G2/M transition. MST3-IN-1 significantly suppressed tumor growth in HepG2 xenograft mice. MST3-IN-1 can be used for the study of liver cancer.
    MST3-IN-1
  • HY-N1414A
    3′,6-Disinapoylsucrose
    		Inhibitor 98.88%
    3′,6-Disinapoylsucrose is a type of oligosaccharide that's effective when taken orally, and it has antidepressant, anti-anxiety, and antioxidant properties. 3′,6-Disinapoylsucrose inhibits neuronal apoptosis by lowering the ratio of Bax to Bcl-2 in hippocampal neurons, and it enhances cognitive function in APP/PS1 transgenic mice by activating the CREB/BDNF signaling pathway.
    3′,6-Disinapoylsucrose
  • HY-15607
    WEHI-539
    		Inhibitor
    WEHI-539 is a selective inhibitor of Bcl-XL with an IC50 of 1.1 nM.
    WEHI-539
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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