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-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-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-114118S3
    Semaglutide-13C6,15N TFA
    Semaglutide-13C6,15N TFA is the 13C- and 15N-labeled Semaglutide TFA (HY-114118A). Semaglutide TFA is a long-acting, selective, competitive, orally active GLP-1R agonist that can penetrate the blood-brain barrier. After activating GLP-1R, Semaglutide TFA promotes insulin secretion, inhibits gastric emptying and appetite, and at the same time enhances autophagy, inhibits oxidative stress and apoptosis. Semaglutide TFA also regulates mitochondrial function and lipid metabolism (such as reducing de novo lipogenesis in the liver). Semaglutide TFA has activities such as lowering blood sugar, reducing weight, neuroprotection (such as improving motor function in Parkinson's disease models, reducing α-synuclein aggregation) and improving hepatic steatosis. Semaglutide TFA can be used for the study of neurodegenerative diseases and liver diseases such as type 2 diabetes, obesity, Parkinson's disease, metabolic associated fatty liver disease (MASLD), and cancer.
    Semaglutide-13C6,15N TFA
  • 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-B1192R
    Estradiol benzoate (Standard)
    Estradiol benzoate (Standard) is the analytical standard of Estradiol benzoate. This product is intended for research and analytical applications. Estradiol benzoate (β-Estradiol 3-benzoate) is a HBx protein inhibitor and inhibits androgen and hepatitis B virus (HBV) transcription, replication. Estradiol benzoate shows antifertility effects, anti- Toxoplasma gondii activity and can improve memory behavior of Ovariectomy (Ovx) female mice.
    Estradiol benzoate (Standard)
  • 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-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-15607
    WEHI-539
    		Inhibitor
    WEHI-539 is a selective inhibitor of Bcl-XL with an IC50 of 1.1 nM.
    WEHI-539
  • 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-112218A
    (R)-MIK665
    		Inhibitor
    (R)-MIK665 is the less active enantiomer of MIK665. MIK665 is a special Mcl-1 inhibitor with an IC50 of 1.81 nM.
    (R)-MIK665
  • HY-138697A
    S65487 sulfate
    		Inhibitor 98.08%
    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-128607
    Mcl1-IN-9
    		Inhibitor
    Mcl1-IN-9 is a potent myeloid cell leukemia-1 (Mcl-1) Inhibitor with an IC50 of 446 nM in reengineered BCR-ABL+ B-ALL cells and a Ki of 0.03 nM.
    Mcl1-IN-9
  • HY-155188
    NWP-0476
    		Inhibitor
    NWP-0476 is BCL-2/BCL-xL inhibitor. NWP-0476 has a modified structure with fine-tuned BCL-xL activity. NWP-0476 can be used for relapsed T-acute lymphoblastic leukemia (T-ALL) research.
    NWP-0476
  • HY-100866
    F1324
    		Inhibitor
    F1324 is a potent, high affinity peptidic inhibitor of B cell lymphoma 6 (BCL6) with an IC50 of 1 nM. F1324 exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI.
    F1324
  • HY-131247
    Bcl-2-IN-2
    		Inhibitor
    Bcl-2-IN-2 is a potent and selective Bcl-2 inhibitor with an IC50 of 0.034 nM and also inhibits Bcl-xL with an IC50 of 43 nM, showing >1000-fold selectivity for Bcl-2 over Bcl-xL.
    Bcl-2-IN-2
  • HY-111537
    rel-AZ5576
    		Inhibitor
    rel-AZ5576 is a selective CDK9 inhibitor with the activity of downregulating Mcl-1 and MYC mRNA transcription and protein expression in diffuse large B-cell lymphoma by inhibiting CDK9, promoting MYC protein turnover, reducing MYC phosphorylation on the stable Ser62 residue and downregulating MYC transcriptional targets, inhibiting the growth of diffuse large B-cell lymphoma cell lines in vitro and in vivo and independent of the cell origin.
    rel-AZ5576
  • HY-156620
    Lacutoclax
    		Inhibitor
    Lacutoclax is a Bcl-2 inhibitor with antineoplastic activity.
    Lacutoclax
  • HY-118874
    Oblimersen
    		Inhibitor
    Oblimersen is a BCL-2 inhibitor targeting BCL-2 RNA. Oblimersen specifically binds to the first six codons of the bcl-2 mRNA sequence, resulting in degradation of bcl-2 mRNA and induces apoptosis by down-regulating expression of Bcl-2. Oblimersen can be used for cancer research.
    Oblimersen
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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