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-112417
    Ki11502
    		Inhibitor 99.30%
    Ki11502 is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that selectively inhibits the activity of PDGF β/α receptors with IC50 values less than 10 nM. Ki11502 selectively inhibits PDGF β receptor phosphorylation, proliferation, and proteoglycan synthesis in human vascular smooth muscle cells. Ki11502 can induce Apoptosis) and exhibits profound antiproliferative effects on select subsets of leukemia, including those with Imatinib (HY-15463) resistant mutations. Ki11502 is highly suitable for studying the role of PDGF in vascular diseases, particularly the role of proteoglycans in atherosclerosis.
    Ki11502
  • HY-153953
    Bcl-2-IN-11
    		Inhibitor
    Bcl-2-IN-11 (compound 6) is a potent and selective Bcl-2 activity inhibitor, with an IC50 of 0.9 nM. Bcl-2-IN-11 shows weak inhibition of Bcl-xl (IC50 > 1000 nM). Bcl-2-IN-11 can be used for the research of a variety of cancers caused by abnormal overexpression of Bcl-2 family proteins: especially malignant hematologic diseases of acute lymphoid leukemia, etc. Bcl-2-IN-11 can also avoid toxic side effects caused by Bcl-xl inhibition, such as thrombocytopenia.
    Bcl-2-IN-11
  • HY-13659
    KRN5500
    		Inhibitor
    KRN5500 (NSC 650426), a Spicamycin (HY-127130) derivative and a nucleoside-like antibiotic with anti-tumor activity. KRN5500 also induces apoptosis via the down-regulation of Bcl-2 expression. KRN5500 shows a significant efficacy in the human tumor xenograft model in mice.
    KRN5500
  • HY-149622
    Bcl-2-IN-12
    		Inhibitor
    Bcl-2-IN-12 (Compound 1) is a Bcl-2 inhibitor (IC50: 6 nM). Bcl-2-IN-12 can be used for cancer research.
    Bcl-2-IN-12
  • HY-149681
    Beclin1-Bcl-2 interaction inhibitor 1
    		Inhibitor
    Beclin1-Bcl-2 interaction inhibitor 1 potently inhibits Beclin 1/Bcl-2 binding. Beclin1-Bcl-2 interaction inhibitor 1 can be used for the research of cancer and neurodegeneration.
    Beclin1-Bcl-2 interaction inhibitor 1
  • HY-124122
    BPTQ
    		Inhibitor
    BPTQ is a potent inhibitor against VEGFR1/Flt-1 and CHK2 with IC50 values of 0.54 and 1.70 µmol/L, respectively. BPTQ is also an intercalator of DNA with anticancer activities. BPTQ inhibits the proliferation of HL-60 cells by arresting cells at S and G2/M phase with an IC50 value of 12 µmol/L. BPTQ also activates the mitochondria-mediated Apoptosis pathway by a decrease in mitochondrial membrane potential, increase in the Bax:Bcl-2 ratio and activation of caspases.
    BPTQ
  • HY-N0361R
    Dihydrocapsaicin (Standard)
    		Modulator
    Dihydrocapsaicin (Standard) is the analytical standard of Dihydrocapsaicin. This product is intended for research and analytical applications. Dihydrocapsaicin, a capsaicin, is a potent and selective TRPV1 (transient receptor potential vanilloid channel 1) agonist. Dihydrocapsaicin reduces AIF, Bax, and Caspase-3 expressions, and increased Bcl-2, Bcl-xL and p-Akt levels. Dihydrocapsaicin enhances the hypothermia-induced neuroprotection following ischemic stroke via PI3K/Akt regulation in rat.
    Dihydrocapsaicin (Standard)
  • HY-159513
    Bcl-2/Mcl-1-IN-4
    		Inhibitor
    Bcl-2/Mcl-1-IN-4 (compound 20) is a dual inhibitor targeting Bcl-2 (Ki=0.49 μM) and Mcl-1 (Ki=0.51 μM). Bcl-2/Mcl-1-IN-4 significantly inhibits cancer cell proliferation and effectively induces apoptosis in U937 cells. Bcl-2/Mcl-1-IN-4 can be used in cancer research.
    Bcl-2/Mcl-1-IN-4
  • HY-170762
    Mcl-1 inhibitor 21
    Mcl-1 inhibitor 21 (Example 1-36) is a Mcl-1 inhibitor with an IC50 of 328 nM. 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-N1904
    4′-Hydroxywogonin
    		Inhibitor
    4′-Hydroxywogonin (8-Methoxyapigenin), a flavonoid, could be isolated from a variety of plants including Scutellaria barbata and Verbena littoralis. 4′-Hydroxywogonin has anti-inflammatory activity via TAK1/IKK/NF-κB, MAPKs and PI3/AKT signaling pathways. 4′-Hydroxywogonin inhibits angiogenesis by disrupting PI3K/AKT signaling. 4′-Hydroxywogonin inhibits cell proliferation and induces apoptosis.
    4′-Hydroxywogonin
  • HY-149978
    LSD1-IN-26
    		Inhibitor
    LSD1-IN-26 (compound 12u) is a potent LSD1 inhibitor, with an IC50 of 25.3 nM. LSD1-IN-26 also inhibits MAO-A (IC50=1234.57 nM) and MAO-B (IC50=3819.27 nM). LSD1-IN-26 significantly induces apoptosis in MGC-803 cells. LSD1-IN-26 can be used for gastric cancer research.
    LSD1-IN-26
  • HY-168739
    Topoisomerase I inhibitor 17
    		Activator
    Topoisomerase I inhibitor 17 (Compound 7h) is a Topoisomerase I (Top1) inhibitor. Topoisomerase I inhibitor 17 reduces DDX5 and reverses the locking of Top1 activity by DDX5. Topoisomerase I inhibitor 17 induces Top1-mediated DNA damage and promotes reactive oxygen species (ROS) production. Topoisomerase I inhibitor 17 induces Apoptosis (reduces antiapoptotic proteins XIAP, Bcl-2, Survivin and up-regulates pro-apoptotic proteins Bax, γH2AX). Topoisomerase I inhibitor 17 also blocks the progression of the G2/M checkpoint and induces cell cycle arrest. Topoisomerase I inhibitor 17 significantly inhibits colony formation and cell migration in colorectal cancer cells. Topoisomerase I inhibitor 17 effectively reduces tumors in human PDX tumor mice.
    Topoisomerase I inhibitor 17
  • HY-169243
    BCL-XL-IN-1
    		Inhibitor
    BCL-XL-IN-1 (Compound 11) is a selective BCL-XL inhibitor with a Ki of <0.01 nM for BCL-XL TR-FERT. BCL-XL-IN-1 can be used in cancer research.
    BCL-XL-IN-1
  • HY-115928
    M24
    		Inhibitor
    M24 is a Mcl-1 selective inhibitor. M24 exhibits good binding affinity against Mcl-1 with Ki value of 0.33 μM. M24 exhibits good anti-proliferative activity and induce apoptosis in HepG2 cells.
    M24
  • HY-144430
    Bcl-2/Mcl-1-IN-1
    		Inhibitor
    Bcl-2/Mcl-1-IN-1 (compound 3) is a Bcl-2/Mcl-1 inhibitor, with Kis of 1.19 μM and 4.53 μM for Mcl-1 and Bcl-2, respectively. Bcl-2/Mcl-1-IN-1 can be used for the research of cancer.
    Bcl-2/Mcl-1-IN-1
  • HY-129159
    (-)-Clerosterol
    (-)-Clerosterol is a natural product that can be isolated from Codium fragile.
    (-)-Clerosterol
  • HY-N0307R
    Ciwujianoside B (Standard)
    		Inhibitor
    Ciwujianoside B (Standard) is the analytical standard of Ciwujianoside B. This product is intended for research and analytical applications. Ciwujianoside B is isolated from Eleutherococcus senticosus leaf, is able to penetrate and work in the brain after the oral administration. Ciwujianoside B significantly enhances object recognition memory. Ciwujianoside B shows radioprotective effects on the hematopoietic system in mice, which is associated with changes in the cell cycle, reduces DNA damage and down-regulates the ratio of Bax/Bcl-2 in bone marrow cells exposed to radiation.
    Ciwujianoside B (Standard)
  • HY-18628S
    UMI-77-d4
    		Inhibitor
    UMI-77-d4 is the deuterium labeled UMI-77. UMI-77 is a selective Mcl-1 inhibitor, which shows high binding affinity to Mcl-1 (IC50=0.31 μM). UMI-77 binds to the BH3 binding groove of Mcl-1 with Ki of 490 nM, showing selectivity over other members of anti-apoptotic Bcl-2 members.
    UMI-77-d<sub>4</sub>
  • HY-146444
    Anticancer agent 56
    		Inhibitor
    Anticancer agent 56 (compound 4d) is a potent anti-cancer agent with agent-likeness properties, possessing anticancer activity against several cancer cell lines (IC50<3 μM). Anticancer agent 56 induces cell cycle arrest at G2/M phase and triggers mitochondrial apoptosis pathway. Anticancer agent 56 acts by accumulation of ROS, up regulation of BAX, down regulation of Bcl-2 and activation of caspases 3, 7, 9.
    Anticancer agent 56
  • HY-147514
    Anticancer agent 64
    		Modulator
    Anticancer agent 64 (compound 5m) shows cytotoxic activity in CCRF-CEM cells, with IC50 of 2.4 μM. Anticancer agent 64 shows good anticancer activity through apoptosis induction. Anticancer agent 64 induces caspase 3 and 7 activation and PARP cleavage. Anticancer agent 64 induces significant effect of mitochondria depolarization.
    Anticancer agent 64
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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