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-148203
    Mcl-1 inhibitor 9
    		Inhibitor
    Mcl-1 inhibitor 9 (example 2) is a myeloid cell leukemia 1 (Mcl-1) inhibitor with IC50 value of 0.21889 nM. Mcl-1 inhibitor 9 shows anti-tumor activity.
    Mcl-1 inhibitor 9
  • HY-153096
    OICR12694
    		Inhibitor
    OICR12694 (JNJ-65234637) is an orally active inhibitor of B cell lymphoma 6 (BCL6).
    OICR12694
  • HY-17510R
    Gossypol (acetic acid) (Standard)
    		Inhibitor
    Gossypol (acetic acid) (Standard) is the analytical standard of Gossypol (acetic acid). This product is intended for research and analytical applications. Gossypol acetic acid ((±)-Gossypol-acetic acid) 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 (acetic acid) (Standard)
  • HY-13846
    BM-1074
    		Inhibitor
    BM-1074 is a potent and specific Bcl-2/Bcl-xL inhibitor with Ki values of < 1 nM and IC50 values of 1.8 nM and 6.9 nM for Bcl-2 and Bcl-xL, respectively. BM-1074 induces apoptosis, and exhibits antiproliferative activity against four small-cell lung cancer cell lines (H146, H1963, H187 and H1417) with IC50 values of 1-2 nM.
    BM-1074
  • HY-P5327
    r8 Bid BH3
    r8 Bid BH3 is a biological active peptide. (The Bid BH3 is a pro-apoptotic member of the 'BH3-only' subset of BCL-2 family proteins that constitute a critical control point in apoptosis. r8BIDBH3 is lethal to human leukemia cell lines that expresse Bcl-2. The Bcl-2 antagonists may have the potential to be efficacious in cancer therapy. Poly-D-arginine (d-isomer as denoted by rrrrrrrr) is fused to the Bid BH3 peptide to facilitate cellular uptake of the peptide.)
    r8 Bid BH3
  • HY-101996
    SMBA1
    		Agonist
    SMBA1 is a potent Bax agonist with a Ki value of 43.3 nM. SMBA1 enhances the Bax expression. SMBA1 shows anti-tumor activity. SMBA1 has the potential for the research of lung cancer.
    SMBA1
  • 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
    BCL2L1 Human Pre-designed siRNA Set A
  • HY-161733
    GQN-B37-Me
    		Inhibitor
    GQN-B37-Me is a MCL-1 inhibitor. GQN-B37-Me induces caspase-dependent apoptosis. GQN-B37-Me exhibits noteworthy cytotoxicity in H929 (IC50 = 3.71 μM) and MV-4-11 (IC50 = 5.57 μM) cells. GQN-B37-Me can be used for the research of leukemia.
    GQN-B37-Me
  • HY-161577
    BFC1103
    BFC1103 is a small-molecule compound whose primary mechanism of action involves interaction with a specific domain of Bcl-2, particularly its loop domain. This interaction induces a conformational change in Bcl-2, exposing its BH3 (Bcl-2 homology 3) domain, thereby switching Bcl-2's function from anti-apoptotic to pro-apoptotic. The cell death induced by BFC1103 is dependent on the presence of Bax or Bak, both of which are key proteins involved in the intrinsic apoptotic pathway mediated by mitochondria. BFC1103 has successfully inhibited lung metastasis of triple-negative breast cancer in mouse models. It can be utilized in studying the roles of Bcl-2 family proteins in cancer development and how they impact the survival and proliferation of cancer cells.
    BFC1103
  • HY-170406
    BCL-XL-IN-3
    		Inhibitor
    BCL-XL-IN-3 (Compound 11) is an inhibitor for BCL-XL with a Ki < 0.01 nM. BCL-XL-IN-3 inhibits the cell viability in normal Molt-4 and Digitonin (HY-N4000)-permeabilized Molt-4 with EC50 of 77.8 nM and 0.07 nM. BCL-XL-IN-3 can be used as ADC toxin for synthesis of Clezutoclax (HY-137774).
    BCL-XL-IN-3
  • 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-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-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-N12960
    Artobiloxanthone
    		Inhibitor
    Artobiloxanthone (Compound AA3) exhibits antitumor activity, particularly against oral squamous cell carcinoma (OSCC). Artobiloxanthone inhibits Akt/mTOR pathway and STAT3 pathway, inhibits proliferation of SAS and T.Tn (with IC50 of 11 and 22 μM), and inhibits the cancer cell migration. Artobiloxanthone arrests cell cycle at S phase, and induces apoptosis in OSCC cells through activation of caspase 3/9.
    Artobiloxanthone
  • 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-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
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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