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-N0307
    Ciwujianoside B
    		Inhibitor 99.68%
    Ciwujianoside B is isolated from Eleutherococcus senticosus leaf, is able to penetrate and work in the brain after the oral administration. Ciwujianoside B significantly enhances object recognition memory. Ciwujianoside B shows radioprotective effects on the hematopoietic system in mice, which is associated with changes in the cell cycle, reduces DNA damage and down-regulates the ratio of Bax/Bcl-2 in bone marrow cells exposed to radiation.
    Ciwujianoside B
  • HY-169172
    Bfl-1-IN-5
    		Inhibitor
    Bfl-1-IN-5 (Compound (R,R,S)-26) is a selective inhibitor for Bfl-1 with an IC50 of 0.022 μM. Bfl-1-IN-5 promotes the caspase-3/7 activity with an EC50 of 0.37 μM, and inhibits the cell viability of SU-DHL-1 with an EC50 of 1.3 μM.
    Bfl-1-IN-5
  • HY-139304
    PROTAC Bcl-xL ligand-1
    		Inhibitor 99.06%
    PROTAC Bcl-xL ligand-1 is a ligand for Bcl-xL that can be used in the synthesis of PROTACs.
    PROTAC Bcl-xL ligand-1
  • HY-N0429
    Diosbulbin B
    		Inhibitor 99.90%
    Diosbulbin B, a diterpene lactone, is an anticancer agent. Diosbulbin B is an orally active component of Dioscorea. bulbifera L. Diosbulbin B can inhibit cell proliferation, induce G0/G1 phase arrest and apoptosis. Diosbulbin B can induce autophagy and mitochondrial dysfunction. Diosbulbin B can induce liver injury. Diosbulbin B can be used for the research of cancer, such as non-small cell lung cancer (NSCLC).
    Diosbulbin B
  • HY-169925
    BM-962
    		Inhibitor 99.10%
    BM-962 (Compound 31) is a potent small-molecule inhibitor of Bcl-2 with an IC50 value of 4 nM (Ki=0.8 nM) and Bcl-xL with an IC50 value of 3.9 nM (Ki <1 nM). BM-962 inhibits the cell growth in H1417 and H146 cell lines with IC50 values of 9 and 13 nM, respectively. BM-962 is promising for research of cancers.
    BM-962
  • HY-111954
    (+)-Erinacin A
    		99.97%
    (+)-Erinacin A (Erinacine A) is a cyanoditerpenoid isolated from Hericium erinaceus with anticancer, anti-inflammatory and neuroprotective activities. (+)-Erinacin A can induce cancer cell death by activating extrinsic and intrinsic apoptosis pathways. (+)-Erinacin A can also inhibit the expression of NO synthase (iNOS) and the production of nitrotyrosine to exert inflammatory and neuroprotective effects, thereby reducing ischemic brain damage.
    (+)-Erinacin A
  • 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-15191B
    (S)-Sabutoclax
    		Inhibitor 98.03%
    (S)-Sabutoclax ((S)-BI-97C1), an optically pure apogossypol derivative, is pan-active inhibitor of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins. (S)-Sabutoclax (Compound II) inhibits the binding of BH3 peptides to Bcl-XL, Bcl-2, Mcl-1, and Bfl-1 with IC50 values of 0.31, 0.32, 0.20, and 0.62 μM, respectively. (S)-Sabutoclax also potently inhibits cell growth of human prostate cancer, lung cancer, and lymphoma cell lines with EC50 values of 0.13, 0.56, and 0.049 μM, respectively. (S)-Sabutoclax can be used for the research of apoptosis-based therapies against cancer.
    (S)-Sabutoclax
  • HY-RS01415
    BCL2 Human Pre-designed siRNA Set A
    		Inhibitor

    BCL2 Human Pre-designed siRNA Set A contains three designed siRNAs for BCL2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    BCL2 Human Pre-designed siRNA Set A
  • HY-W654330
    Pyraclostrobin-d6
    		99.90%
    Pyraclostrobin-d6 is deuterium-labeled Pyraclostrobin (HY-N6626).
    Pyraclostrobin-d<sub>6</sub>
  • HY-161242A
    CBI1 formic
    		Inhibitor
    CBI1 formic is a covalent BAX inhibitor. CBI1 formic selectively derivatizes BAX at C126 and inhibits BAX activation by triggering ligands or point mutagenesis. CBI1 formic blocks t-2-hex lipidation and oligomerization of BAX. CBI1 formic inhibits BAX activation induced by BH3 ligands, F116A mutagenesis or t-2-hex.
    CBI1 formic
  • HY-109617
    4-(4-Fluorophenyl)benzoic acid
    		99.01%
    4-(4-Fluorophenyl)benzoic acid (Compoud 6) can bind to Bcl-2 with a KD value of 400 μM. 4-(4-Fluorophenyl)benzoic acid can be used to develope Bcl-2 selective anti-cancer agent.
    4-(4-Fluorophenyl)benzoic acid
  • HY-117288A
    S55746 hydrochloride
    		Inhibitor 99.66%
    S55746 hydrochloride (BCL201 hydrochloride) is a potent, orally active and selective BCL-2 inhibitor, with a Ki of 1.3 nM and a Kd of 3.9 nM. S55746 hydrochloride (BCL201 hydrochloride) has antitumor activity with low toxicity.
    S55746 hydrochloride
  • HY-138697A
    S65487 sulfate
    		Inhibitor 99.35%
    S65487 (VOB560) sulfate, a potent and selective Bcl-2 inhibitor, is a proagent of S55746. S65487 sulfate is also active on BCL-2 mutations, such as G101V and D103Y. S65487 sulfate has poor affinity with MCL-1, BFL-1 and BCL-XL. S65487 sulfate induces apoptosis and has anticaner activities.
    S65487 sulfate
  • HY-138697B
    S65487 hydrochloride
    		Inhibitor 99.67%
    S65487 (VOB560) hydrochloride, a potent and selective Bcl-2 inhibitor, is a proagent of S55746. S65487 hydrochloride is also active on BCL-2 mutations, such as G101V and D103Y. S65487 hydrochloride has poor affinity with MCL-1, BFL-1 and BCL-XL. S65487 hydrochloride induces apoptosis and has anticaner activities.
    S65487 hydrochloride
  • HY-10969A
    Obatoclax
    		Inhibitor ≥99.0%
    Obatoclax (GX15-070), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2. Obatoclax induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax has anti-cancer and broad-spectrum antiparasitic activity.
    Obatoclax
  • HY-19551
    Apogossypolone
    		Inhibitor 98.58%
    Apogossypolone (ApoG2) is an orally active Bcl-2 family proteins inhibitor with Ki values of 35, 25 and 660 nM for Bcl-2, Mcl-1 and Bcl-XL, respectively. Apogossypolone shows antitumor activities, induces cell apoptosis and autophagy. Apogossypolone also has antifungal activity.
    Apogossypolone
  • HY-136640
    BCL6-IN-4
    		Inhibitor 99.72%
    BCL6-IN-4 is a potent B-cell lymphoma 6 (BCL6) inhibitor with an IC50 of 97 nM. BCL6-IN-4 has anti-tumor activities.
    BCL6-IN-4
  • HY-119368
    NPB
    		Inhibitor 98.0%
    NPB is a specific and potent inhibitor of BAD phosphorylation at Ser99, with an IC50 of 0.41 μM.
    NPB
  • HY-161276
    BFC1108
    		98.11%
    BFC1108 is a small molecule Bcl-2 functional converter. BFC1108 induces a conformational change in Bcl-2, resulting in the exposure of its BH3 domain both in vitro and in vivo. BFC1108 effectively induces apoptosis in Bcl-2 expressing cancers..
    BFC1108
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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