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-154962
    Mcl-1 inhibitor 15
    		Inhibitor
    Mcl-1 inhibitor 15 (Compound (Ra)-15) is a Mcl-1 inhibitor (Ki: 0.02 nM). Mcl-1 inhibitor 15 can be used for research of cancer.
    Mcl-1 inhibitor 15
  • HY-175815
    Apoptosis inducer 44
    		Inhibitor
    Apoptosis inducer 44 is an apoptosis inducer. Apoptosis inducer 44 triggers apoptosis in MDA-MB-231 cells by increasing the levels of Bax and Cyt C, reducing Bcl-2, and initiating caspase-3 cleavage. Apoptosis inducer 44 suppresses the invasion and migration of MDA-MB-231 cells by down-regulating MMP-2 and MMP-9 expression and up-regulating E-cadherin protein levels. Apoptosis inducer 44 can be used for the study of breast cancer.
    Apoptosis inducer 44
  • HY-161874
    RPS6-IN-1
    		Inducer
    RPS6-IN-1 (Compound 22o) inhibits cell metastasis, induces cell apoptosis (increases the expression of Bax, p53, cleaved-caspase 3, and cleaved-PARP). RPS6-IN-1 decreases mitochondrial membrane potential. RPS6-IN-1 activates autophagy through the PI3K-Akt-mTOR signaling pathway, damages intracellular mitochondria and lysosomes, and cause ER stress. RPS6-IN-1 inhibits RPS6 phosphorylation. RPS6-IN-1 is an anticancer agent with low systemic toxicity.
    RPS6-IN-1
  • HY-148899
    Mcl-1 inhibitor 10
    		Inhibitor
    Mcl-1 inhibitor 10 (compound 43) is a relatively strong MCL-1 inhibitor (IC50=0.67 μM). Mcl-1 inhibitor 10 interacts with specific binding sites of MCL-1 protein to block the pro-survival signal of MCL-1 and push cancer cells into apoptosis. Mcl-1 inhibitor 10 can be used in the study of MCL-1 dependent cancers.
    Mcl-1 inhibitor 10
  • HY-10087A1
    Navitoclax dihydrochloride
    		Inhibitor
    Navitoclax (ABT-263) dihydrochloride is an orally active Bcl-2 inhibitor that binds to various Bcl-2 family proteins, including Bcl-xL, Bcl-2, and Bcl-w, with a Ki value of less than 1 nM. Navitoclax dihydrochloride can be used in cancer research.
    Navitoclax dihydrochloride
  • HY-17495
    Carteolol
    		Activator
    Carteolol is a non-selective β-adrenoceptor antagonist. Carteolol induces apoptosis via a caspase activated and mitochondrial-dependent pathway. Carteolol can be used for glaucoma research.
    Carteolol
  • HY-N6626R
    Pyraclostrobin (Standard)
    Pyraclostrobin (Standard) is the analytical standard of Pyraclostrobin. This product is intended for research and analytical applications. Pyraclostrobin is a highly effective and broad-spectrum strobilurin fungicide. Pyraclostrobin can induce oxidative DNA damage, mitochondrial dysfunction and autophagy through the activation of AMPK/mTOR signaling. Pyraclostrobin can be used to control crop diseases.
    Pyraclostrobin (Standard)
  • HY-175608
    EGFR-IN-171
    		Inhibitor
    EGFR-IN-171 is an EGFR inhibitor with an IC50 value of 0.19 μM. EGFR-IN-171 also inhibits vascular endothelial growth factor 2 (VEGFR-2) with an IC50 value of 31.65 μM. EGFR-IN-171 can induce apoptosis and G2/M phase cell cycle arrest. EGFR-IN-171 can be used for cancer research, such as liver and breast cancer.
    EGFR-IN-171
  • 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-129488
    FPFS-1169 hydrochloride
    		Agonist
    FPFS-1169 (hydrochloride) is a proto-oncogene protein c-bcl-2 stimulant. FPFS-1169 (hydrochloride) can increase the impulse-evoked release of monoamine neurotransmitters. FPFS-1169 (hydrochloride) can be studied in research on Parkinson’s disease.
    FPFS-1169 hydrochloride
  • 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-175257
    Theophylline-platinum(IV) prodrug-1
    		Inhibitor
    Theophylline-platinum(IV) prodrug-1 is a PARP-1 inhibitor. Theophylline-platinum(IV) prodrug-1 enhances DNA damage, ROS production, mitochondrial dysfunction, apoptosis and S-phase arrest, along with reducing invasion and metastasis in cells. Theophylline-platinum(IV) prodrug-1 exhibits superior antitumor activity in the xenograft SKOV3-BRCA1-KD tumor model. Theophylline-platinum(IV) prodrug-1 can be used for the study of ovarian cancer.
    Theophylline-platinum(IV) prodrug-1
  • HY-177076
    Dalvotoclax
    		Inhibitor
    Dalvotoclax (Example 8) is a selective inhibitor of BCL-2. Dalvotoclax has good liver microsomal stability. Dalvotoclax inhibits the activity of anti-apoptotic BCL-2 protein and anti-apoptotic BCL-XL protein. Dalvotoclax can be studied in research for B cell leukemia.
    Dalvotoclax
  • HY-P11198
    AC-P19M
    		Inhibitor
    AC-P19M is an anticancer peptide. AC-P19M induces apoptosis by disrupting the cell membrane of cancer cells. AC-P19M reverses epithelial-mesenchymal transition (EMT). AC-P19M shows anti-angiogenic activity through the inhibition of VEGF-VEGFR2/ERK/Akt signaling. AC-P19M can be used for lung cancer research.
    AC-P19M
  • 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-N15449
    Vicanicin
    		Inhibitor
    Vicanicin is a depsidone compound found in lichens. Vicanicin inhibits the expression of Hsp70, regulates the redox-sensitive mechanisms within cells, promotes the increase of reactive oxygen species (ROS) in cancer cells, changes the Bax/Bcl-2 ratio, activates caspase-3, and triggers apoptosis. Vicanicin inhibits cell growth and induces apoptosis in androgen-sensitive (LNCaP) and androgen-insensitive (DU-145) human prostate cancer cells. Vicanicin is promising for research of prostate cancer.
    Vicanicin
  • 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
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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