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-100763
    Mcl1-IN-12
    		Inhibitor
    Mcl1-IN-12 (Compound F) is a selective Mcl-1 inhibitor, less potent at Bcl-2, with Kis of 0.29 and 3.1 μM, respectively. Anti-tumor activity.
    Mcl1-IN-12
  • HY-133015
    Mcl-1 inhibitor 3
    		Inhibitor
    Mcl-1 inhibitor 3 (compound 1) is a highly potent and orally activate macrocyclic Mcl-1 inhibitor (Ki= 0.061 nM; IC50=19 nM in an OPM-2 cell viability assay). Mcl-1 inhibitor 3 shows good pharmacokinetic properties and excellent in vivo efficacy without toxicity.
    .
    Mcl-1 inhibitor 3
  • HY-B0402B
    Amantadine sulfate
    		Modulator
    Amantadine (1-Adamantanamine) sulfate is an orally avtive and potent antiviral agent with activity against influenza A viruses. Amantadine sulfate inhibits several ion channels such as NMDA and M2, and also inhibits Coronavirus ion channels. Amantadine sulfate also has anti-orthopoxvirus and anticancer activity. Amantadine sulfate can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research.
    Amantadine sulfate
  • HY-117235R
    Diallyl Trisulfide (Standard)
    		Activator
    Diallyl Trisulfide (Standard) is the analytical standard of Diallyl Trisulfide. This product is intended for research and analytical applications. Diallyl Trisulfide is an orally active anticancer agent that can be isolated from garlic. Diallyl Trisulfide has the ability to induce apoptosis and exhibits anticancer, anti-inflammatory, antioxidant, and antibacterial activities. Diallyl Trisulfide can be used to study a variety of cancers, including liver, colon and prostate cancer[1][2][3][4].
    Diallyl Trisulfide (Standard)
  • HY-18106
    BM 957
    		Inhibitor
    BM 957 is a potent Bcl-2 and Bcl-xL inhibitor, with Kis of 1.2, <1 nM and IC50s of 5.4, 6.0 nM respectively.
    BM 957
  • HY-P2499
    BAD (103-127) (human), FAM-labeled
    		Inhibitor
    BAD (103-127) (human), FAM-labeled is a FAM-labeled human BAD (103-127) (HY-P2468). BAD (103-127) (human), the 25-mer Bad peptide, is derived from the BH3 domain of BAD and can antagonize the function of Bcl-xL.
    BAD (103-127) (human), FAM-labeled
  • HY-N1440R
    Koumine (Standard)
    		Activator
    Koumine (Standard) is the analytical standard of Koumine. This product is intended for research and analytical applications. Koumine is an alkaloid separated from Gelsemium elegans, shows potent anti-tumor activity. Koumine up-regulates the Bax/Bcl-2 ratio and caspase-3 expression in human breast cancer cells. Koumine has anxiolytic, antistress, antipsoriatic, and analgesic activities, protects against the development of arthritis in Rheumatoid arthritis (RA) animal models.
    Koumine (Standard)
  • HY-153423
    Mcl-1 inhibitor 12
    		Inhibitor
    Mcl-1 inhibitor 12 (Example 10) is a MCL-1 inhibitor (Ki: 0.22 nM). Mcl-1 inhibitor 12 can be used for the research of cancers.
    Mcl-1 inhibitor 12
  • HY-174403
    c-MYC/BCL2 ligand 1 iodide
    		Ligand
    c-MYC/BCL2 ligand 1 iodide is a dual-targeting c-MYC/Bcl-2 G4 ligand with Kd values of 0.90 μM (c-MYC G4) and 0.56 μM (Bcl-2 G4). c-MYC/BCL2 ligand 1 iodide inhibits c-MYC and Bcl-2 gene transcription by binding to G4-forming sequences and downregulates their protein expression. c-MYC/BCL2 ligand 1 iodide inhibits suppresses migration, induces caspase-dependent apoptosis, and triggers cell cycle G1 arrest in MCF-7 cells. c-MYC/BCL2 ligand 1 iodide significantly suppresses tumor growth in a 4T1 syngeneic model with no observable toxicity. c-MYC/BCL2 ligand 1 iodide can be used for the research of breast cancer.
    c-MYC/BCL2 ligand 1 iodide
  • HY-146183
    BCL6-IN-9
    		Inhibitor
    BCL6-IN-9 (compound 1) is a potent B-cell lymphoma 6 protein (BCL6) inhibitor, with an IC50 of 3.9 nM. BCL6-IN-9 can be used for the research of cancer.
    BCL6-IN-9
  • HY-RS01358
    Bak1 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Bak1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Bak1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Bak1 Mouse Pre-designed siRNA Set A
  • HY-170648
    TS-IN-5
    		Modulator
    TS-IN-5 (Compound 15) is a thymidylate synthase (TS) inhibitor. TS-IN-5 induces Apoptosis by modulating Bax, BCL-2, PI3K, and STAT1 proteins. TS-IN-5 shows antitumor effects against liver, breast and colon cancers.
    TS-IN-5
  • HY-P5341
    Bik BH3
    Bik BH3 is a biological active peptide. (BH3 domain of BIK)
    Bik BH3
  • HY-155012
    Mcl-1 inhibitor 16
    		Inhibitor
    Mcl-1 inhibitor 16 (Compound 9) is a mitochondrial targeting Platinum-based inhibitor of Mcl-1. Mcl-1 inhibitor 1 induces Bax/Bak-dependent apoptosis in cancer cells. Mcl-1 inhibitor 16 can be used alone or together with ABT-199 (HY-15531) and shows anti-tumor activity.
    Mcl-1 inhibitor 16
  • HY-N2741
    Vitexin B-1
    		Inhibitor
    Vitexin B-1 is an inhibitor of Bcl-2 and the agonist of Caspase. Vitexin B-1 has cytotoxic effect and induces apoptosis in MCF-7, ZR-75-1, MDA-MB-231, and COC1 cells with IC50s of 3.2, 2.1, 1.8 and 0.39 μM, respectively.
    Vitexin B-1
  • HY-N0831R
    Jaceosidin (Standard)
    		Activator
    Jaceosidin (Standard) is the analytical standard of Jaceosidin. This product is intended for research and analytical applications. Jaceosidin is a flavonoid isolated from Artemisia vestita, induces apoptosis in cancer cells, activates Bax and down-regulates Mcl-1 and c-FLIP expression. Jaceosidin exhibits anti-cancer, anti-inflammatory activities, decreases leves of inflammatory markers, and suppresses COX-2 expression and NF-κB activation.
    Jaceosidin (Standard)
  • HY-159817
    Asaretoclax
    		Inhibitor
    Asaretoclax is a potent B-cell lymphoma 2 (Bcl-2) inhibitor. Asaretoclax has the potential for the research of cancer.
    Asaretoclax
  • HY-175236
    SF-9-2
    		Inhibitor
    SF-9-2 is a PD-L1/PD-1 binding inhibitor (IC50 = 24.9 nM). SF-9-2 inhibits epithelial-mesenchymal transition, migration, invasion, and proliferation of SK-N-SH cells, and also induces apoptosis and cell cycle arrest. SF-9-2 blocks PD-L1-induced SK-N-SH cell growth through the MAPK signaling pathway. SF-9-2 restores GSK-3β activity and enhances PD-L1 degradation through the ubiquitin-proteasome pathway. SF-9-2 inhibits tumor growth in the SK-N-SH NOG mouse model without significant toxicity. SF-9-2 also acts as an immune checkpoint inhibitor, blocking PD-L1 to restore T cell function. SF-9-2 can be used in neuroblastoma research.
    SF-9-2
  • HY-178176
    PROTAC CB1R Degrader-1
    		Inhibitor
    PROTAC CB1R Degrader-1 is a potent and selective CB1R PROTAC degrader that exploits the ubiquitin-proteasome system (UPS) achieving a DC50 of 3.37 μM in MCF-7 cells and showing no impact on CB2R. PROTAC CB1R Degrader-1 reduces CB1R-associated downstream signaling (p-AKT, p-ERK, BCL2, and MCM5), thereby inhibiting breast cancer cell proliferation and inducing apoptosis. PROTAC CB1R Degrader-1 can be used for breast cancer research. (Blue: CRBN ligand (HY-41547); Black: linker (HY-178198); Pink: CB1R ligand (HY-134497)).
    PROTAC CB1R Degrader-1
  • HY-122721
    Mcl1-IN-5
    		Inhibitor
    Mcl1-IN-5 (compound 21) is a MCL-1 inhibitor. Mcl1-IN-5 can be used for the research of cancers.
    Mcl1-IN-5
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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