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-162008
    S1g-10
    		Inhibitor
    S1g-10 is a Hsp70/Bim inhibitor, and shows antitumor activity in chronic myeloid leukemia cells.
    S1g-10
  • HY-143873
    Bcl-2-IN-5
    		Inhibitor
    Bcl-2-IN-5 is a BCL-2 inhibitor with IC50s of 0.12 nM, 0.14 nM and 0.22 nM for Bcl-2 wild type, Bcl-2 D103Y and Bcl-2 G101V, respectively. Bcl-2-IN-5 inhibits the cell growth with IC50 values of 0.2 nM and 0.44 nM for Bcl 2-G101V knock-in RS4; 11 and RS4; 11 cells, respectively (WO2021208963A1; Example 155).
    Bcl-2-IN-5
  • HY-155242
    VEGFR-2-IN-36
    		Modulator
    VEGFR-2-IN-36 (compound 15) is a VEGFR-2 inhibitor (IC50: 0.067 μM) and inducer of apoptosis with anticancer activity. VEGFR-2-IN-36 upregulates BAX levels and downregulates Bcl-2 levels. VEGFR-2-IN-36 is toxic to cancer cells, MCF-7 (IC50=0.42 μM) and HepG2 (IC50=0.22 μM).
    VEGFR-2-IN-36
  • HY-164453
    A-1248767
    A-1248767 is a MCL-1 inhibitor (IC50=23.9 nM; Ki=0.41 nM) with anticancer activity. A-1248767, a derivative of A-1210477 (HY-12468), binds to MCL-1 with high affinity, induces the increase of intracellular MCL-1 protein, and promotes tumor cell apoptosis.
    A-1248767
  • HY-153494A
    Rosomidnar sodium
    		Inhibitor
    PNT100 sodium is a 24-base, chemically unmodified DNA oligonucleotide sequence that is complementary to the regulatory region upstream of the BCL-2 gene. Exposure of tumor cells to PNT100 results in suppression of proliferation and cell death.
    Rosomidnar sodium
  • HY-153423A
    Mcl-1 inhibitor 13
    		Inhibitor
    Mcl-1 inhibitor 13 (Example 9) is a MCL-1 inhibitor (Ki: 8.2 nM). Mcl-1 inhibitor 13 can be used for the research of cancers.
    Mcl-1 inhibitor 13
  • HY-163854
    HSP70-IN-6
    		Inhibitor
    HSP70-IN-6 (Compound JL-15) is an inhibitor of Hsp70-Bim protein-protein interaction (PPI) (IC50: 70 nM). HSP70-IN-6 induces apoptosis in chronic myeloid leukemia (CML) cells, with EC50s of 0.43 μM(BV173), 0.88 μM (K562), 0.19 μM (K562-R3).
    HSP70-IN-6
  • HY-169244
    CDK-TCIP1
    		Inhibitor
    CDK-TCIP1 is a bivalent molecule linking CDK9 inhibitor SNS-032 (HY-10008) to BCL6 ligand BI3812 (HY-111381). CDK-TCIP1 potently and specifically kills BCL6-overexpressing cells with EC50 of 7.7 nM for SUDHL5 cells.
    CDK-TCIP1
  • HY-148368
    CYD-4-61
    		Activator
    CYD-4-61 is a novel Bax activator used for breast cancer research. CYD-4-61 inhibits triple-negative breast cancer MDA-MB-231 and ER-positive breast cancer MCF-7 cell lines proliferation. CYD-4-61 activates Bax protein to induce cytochrome c release and regulate apoptotic biomarkers, leading to cancer cell apoptosis.
    CYD-4-61
  • HY-175010
    STAT3-IN-44
    		Inhibitor
    STAT3-IN-44 is a potent STAT3 inhibitor with IC50s of 1.84 (C6 cells) and 4.81 μM (A549 cells). STAT3-IN-44 inhibits STAT3 phosphorylation, downregulates Bcl-2, and upregulates Caspase-3 to promote late-stage apoptosis. STAT3-IN-44 significantly suppresses tumor cell proliferation and migration. STAT3-IN-44 can be used for the study of cancers such as glioma and lung cancer.
    STAT3-IN-44
  • HY-N2575R
    Hypocrellin A (Standard)
    Hypocrellin A (Standard) is the analytical standard of Hypocrellin A. This product is intended for research and analytical applications. Hypocrellin A is a PKC inhibitor that exerts antidiabetic activity by reversing the effects of high glucose on endothelin (ET-1) expression. Hypocrellin A is also a photosensitizer for photodynamic therapy (PDT) with anticancer, antibacterial and antiviral activities, especially against human immunodeficiency virus (HIV). In addition, Hypocrellin-A also possesses anti-Leishmania activity (IC50=0.27 μg/ml)[1][2][3][4][5][6][7][8][9].
    Hypocrellin A (Standard)
  • HY-144791
    Bcl-2-IN-6
    		Modulator
    Bcl-2-IN-6 (compound 10) is a potent Bcl-2 (B-cell lymphoma-2) inhibitor. Bcl-2-IN-7 down-regulates the expression of Bcl-2, and increases the expression of p53, Bax, and caspase-7 mRNA. Bcl-2-IN-7 induces cell cycle arrest and apoptosis in breast cancer MCF-7 cells. Bcl-2-IN-7 shows good anticancer activity, with IC50 values of 20.91, 22.30, 42.29, and 48.00 μM against MCF-7, LoVo, HepG2, and A549 cell lines, respectively.
    Bcl-2-IN-6
  • HY-172623
    EGFR/HER2-IN-17
    		Inhibitor
    EGFR/HER2-IN-17 (Compound 7h) is a dual inhibitor of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2). EGFR/HER2-IN-17 inhibits cancer cell proliferation. EGFR/HER2-IN-17 interacts with the binding pockets of EGFR and HER2, activating caspase-3 and caspase-8, and decreases the expression of Bcl-2, thereby inducing apoptosis. EGFR/HER2-IN-17 is promising for research of cancers.
    EGFR/HER2-IN-17
  • HY-170662
    VEGFR-2-IN-62
    VEGFR-2-IN-62 (Compound 3f) is an effective VEGFR-2 inhibitor with an IC50 value of 0.0557 μM. VEGFR-2-IN-62 can inhibit cell proliferation and induce apoptosis, and can be used in cancer research.
    VEGFR-2-IN-62
  • HY-RS01424
    BCL2L10 Human Pre-designed siRNA Set A
    		Inhibitor

    BCL2L10 Human Pre-designed siRNA Set A contains three designed siRNAs for BCL2L10 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    BCL2L10 Human Pre-designed siRNA Set A
  • HY-158677
    BcI-2/BcI-xI ligand 1
    BcI-2/BcI-xI ligand 1 is a BcI-2/BcI-xI ligand, and can be used for synthesis of PROTAC BcI-2/BcI-xI Degrader-1 (HY-158551).
    BcI-2/BcI-xI ligand 1
  • HY-144431
    Bcl-2/Mcl-1-IN-3
    		Inhibitor
    Bcl-2/Mcl-1-IN-3 (compound 1) is a Bcl-2/Mcl-1 inhibitor, with Kis of 0.14 μM and 0.23 μM for Mcl-1 and Bcl-2, respectively. Bcl-2/Mcl-1-IN-3 can be used for the research of cancer.
    Bcl-2/Mcl-1-IN-3
  • HY-176142
    YX0798
    		Inhibitor
    YX0798 is a selective and orally active CDK9 inhibitor (Kd: 0.28 nM). YX0798 downregulates the oncoprotein c-MYC and pro-survival protein MCL-1. YX0798 disrupts the cell cycle and results in transcriptomic reprogramming, eventually leading to cell apoptosis. YX0798 has antitumor activity.
    YX0798
  • HY-169381
    hMcl-1-IN-1
    		Inhibitor
    hMcl-1-IN-1 (Compound 9) is an hMcl-1 inhibitor based on His224 aryl sulfonate fluoride, with an IC50 value of 5.8 nM.
    hMcl-1-IN-1
  • HY-168983
    Lonitoclax
    		Inhibitor
    Lonitoclax is a B-cell lymphoma 2 (Bcl-2) inhibitor. Lonitoclax has comparable anti-tumor efficacy to Venetoclax (HY-15531) in both B cell and myeloid malignancy models. Lonitoclax is promising for research of relapsed or refractory chronic lymphocytic leukemia (CLL), small lymphocytic lymphoma, and certain low-grade lymphomas.
    Lonitoclax
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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