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-168623
    EGFR-IN-134
    		Inhibitor
    EGFR-IN-134 (compound 3f), a triazolo[3,4-a]isoquinoline derivative, is a potent EGFR inhibitor with an IC50 of 0.023 µM. EGFR-IN-134 induces apoptosis and necrosis. EGFR-IN-134 initiates cell cycle arrest at the G2/M and pre-G1 phases, downregulates anti-apoptotic protein Bcl2 and upregulates pro-apoptotic proteins: p53, Bax, and caspases 3, 8, and 9. EGFR-IN-134 shows antiproliferative and anticancer activity.
    EGFR-IN-134
  • HY-153494
    Rosomidnar
    		Inhibitor
    PNT100 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
  • 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-RS01434
    BCL2L2 Human Pre-designed siRNA Set A
    		Inhibitor

    BCL2L2 Human Pre-designed siRNA Set A contains three designed siRNAs for BCL2L2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    BCL2L2 Human Pre-designed siRNA Set A
  • HY-153594
    Bcl-B inhibitor 1
    		Inhibitor ≥98.0%
    Bcl-B inhibitor 1 is a Bcl-B inhibitor.
    Bcl-B inhibitor 1
  • HY-N0168AR
    (Rac)-Hesperetin (Standard)
    (Rac)-Hesperetin (Standard) is the analytical standard of (Rac)-Hesperetin. This product is intended for research and analytical applications. (Rac)-Hesperetin is the racemate of Hesperetin. Hesperetin is a natural flavanone that can be found in citrus, and acts as a potent and orally active broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation. Hesperetin displays a range of bioactivities including antioxidant, anti-inflammatory, and anti-cancer. Hesperetin is found to induce cell-cycle arrest at G2/M phase. Hesperetin can reduce Bcl-2 and enhance BaxM. Hesperetin induces apoptosis through inhibiting NF-κB receptor.
    (Rac)-Hesperetin (Standard)
  • HY-170763
    Mcl-1 inhibitor 22
    Mcl-1 inhibitor 22 (Example 36) is a myeloid cell leukemia-1 (MCL-1) inhibitor which inhibits the antiapoptotoic activity of MCL-1 by inhibiting its interaction with proapototic proteins. Mcl-1 inhibitor 22 exhibits anti-proliferation activities against various cancer cell lines and can be utilized in cancer research.
    Mcl-1 inhibitor 22
  • HY-174396
    PI3Kδ/HDAC6-IN-1
    		Inhibitor
    PI3Kδ/HDAC6-IN-1 (Compound 22E) is an orally active and dual inhibitor of PI3Kδ and HDAC6 with IC50 values of 2.4 nM and 6.2 nM, respectively. PI3Kδ/HDAC6-IN-1 exhibits potent antiproliferative effects on non-Hodgkin lymphoma (NHL) cells and possesses in vivo antitumor activity without significant toxicity. PI3Kδ/HDAC6-IN-1 arrests the cell cycle at the G0/G1 phase and induces apoptosis. PI3Kδ/HDAC6-IN-1 blocks the PI3K/AKT/mTOR signaling pathway and increases the acetylation levels of α-tubulin and histone H3.
    PI3Kδ/HDAC6-IN-1
  • HY-RS01435
    Bcl2l2 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Bcl2l2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Bcl2l2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Bcl2l2 Mouse Pre-designed siRNA Set A
  • HY-125191
    BRD1991
    		Inhibitor
    BRD1991 selectively disrupts Beclin 1/Bcl-2 binding and induces autophagy without triggering apoptosis or other forms of cell death.
    BRD1991
  • HY-174457
    STAT3/CAIX-IN-1
    		Inhibitor
    STAT3/CAIX-IN-1 is a dual-target inhibitor of STAT3 (Kd: 60.03 μM) and CAIX (IC50: 80.45 nM). STAT3/CAIX-IN-1 induces ferroptosis by increases the levels of reactive oxygen species (ROS) and lipid peroxides. STAT3/CAIX-IN-1 inhibits cell migration, induces apoptosis, and causes cell cycle arrest in MDA-MB-231 cells. STAT3/CAIX-IN-1 can be used for the study of triple-negative breast cancer (TNBC).
    STAT3/CAIX-IN-1
  • HY-113427S
    trans-Vaccenic acid-d13
    		Inhibitor
    trans-Vaccenic acid-d13 is deuterium labeled trans-Vaccenic acid (HY-113427). trans-Vaccenic acid is a naturally occurring trans fatty acid (TFA). trans-Vaccenic acid inhibits nasopharyngeal carcinoma (NPC) cell growth and induces apoptosis through the inhibition of Bad/Akt phosphorylation. trans-Vaccenic acid is a precursor for the synthesis of saturated fatty acid in the rumen and of conjugated Linoleic acid (CLA) at the tissue level. trans-Vaccenic acid exerts hypolipidemic effects in a rat model of obesity.
    trans-Vaccenic acid-d<sub>13</sub>
  • HY-123244
    YC137
    		Antagonist
    YC137 is a potent Bcl-2 antagonist with Kis of 1.3 μM and >100 μM for Bcl-2 and Bcl-xL when assayed in Bis-Tris buffer, respectively. YC137 inhibits the binding of the Bid BH3 peptide to Bcl-2, thus disrupting an interaction essential for the antiapoptotic activity of Bcl-2. YC137 selectively induces apoptosis of Bcl-2-dependent cells. YC137 has the potential for breast cancer research.
    YC137
  • HY-101999
    EM20-25
    		Inhibitor
    EM20-25 is an inhibitor for Bcl-2, which interferes with the interaction between BCL-2 and BAX, activates caspase-9 and thus induces the apoptosis. EM20-25 affects the mitochondrial function, causes the open of permeability transition pore (PTP). EM20-25 enhances the sensitivity of cells to Staurosporine (HY-15141), and enhances the killing effect of BCL-2-expressing leukemia cells to Chlorambucil (HY-13593) and Fludarabine (HY-B0069).
    EM20-25
  • HY-174878
    BCL-xL ligand 2
    		Degrader
    BCL-xL ligand 2 is a ligand for BCL-xL. BCL-xL ligand 2 can be conjugated with E3 ligase Ligand (HY-138793) and linker to synthesize Bcl-xL PROTAC degrader PZ671 (HY-174876).
    BCL-xL ligand 2
  • HY-170762B
    (-)-Mcl-1 inhibitor 21
    (-)-Mcl-1 inhibitor 21 (Example 1-38) is a Mcl-1 inhibitor with an IC50 of 7.51 μM. (-)-Mcl-1 inhibitor 21 exhibits proapototic and anti-proliferation activities against SUDHL5 and SUDHL10 cell lines and can be utilized in cancer research.
    (-)-Mcl-1 inhibitor 21
  • HY-174411
    Tubulin polymerization-IN-82
    		Inhibitor
    Tubulin polymerization-IN-82 is a tubulin inhibitor. Tubulin polymerization-IN-82 inhibits cell migration and invasion, and triggers cell apoptosis through the mitochondria and ER stress mediated pathway. Tubulin polymerization-IN-82 exhibits antitumor activity against drug resistance cancer cells, and inhibits tumor growth, can be used for liver cancer research.
    Tubulin polymerization-IN-82
  • HY-129325
    Cytochalasin H
    		Inhibitor
    Cytochalasin H is a nature product that could be isolated from fungus Phomopsis sp. Cytochalasin H inhibits cell growth and induces apoptosis. Cytochalasin H has anti-angiogenic activity. Cytochalasin H is an antibiotic and has antibacterial activity.
    Cytochalasin H
  • HY-172551
    anti-TNBC agent-9
    		Inhibitor
    anti-TNBC agent-9 (Compound 3as) is an anti-cancer agent for triple-negative breast cancer (TNBC). anti-TNBC agent-9 exhibits significant inhibitory activity against MDA-MB-453 cells with an IC50 value of 8.5 μM. anti-TNBC agent-9 inhibits tumor cell migration by upregulating E-cadherin and downregulating N-cadherin, matrix metalloproteinase 2 (MMP2), and MMP9. anti-TNBC agent-9 induces apoptosis by increasing the expression of the pro-apoptotic protein BAX and decreasing the expression of the anti-apoptotic protein BCL-2, thereby inhibiting tumor cell proliferation.
    anti-TNBC agent-9
  • HY-150596
    CT1-3
    		Inhibitor
    CT1-3 is a potent anticancer agent. CT1-3 induces mitochondria-mediated apoptosis by regulating JNK/Bcl-2/Bax/XIAP pathway. CT1-3 suppresses the epithelial mesenchymal transition (EMT) potential of human cancer cells (HCCs) via regulating the E-cadherin/Snail axis, thus inhibits tumorigenesis. CT1-3 has a strong antitumor effect in mice model and exhibits no significant hepatic and renal toxicity.
    CT1-3
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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