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-148026
    Sonrotoclax
    		Inhibitor 99.61%
    Sonrotoclax is a potent, orally active Bcl2 inhibitor. Sonrotoclax has effective cell killing effect against a variety of lymphoma and leukemia cell lines.
    Sonrotoclax
  • HY-117235
    Diallyl Trisulfide
    		Activator
    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.
    Diallyl Trisulfide
  • HY-B0257
    Levonorgestrel
    		Inhibitor 99.94%
    Levonorgestrel is an orally active inhibitor of progesterone (HY-N0437). Levonorgestrel has anticancer activity and can induce Apoptosis. Levonorgestrel can be used as a contraceptive and in combination with other medications. Levonorgestrel can be used in the study of osteoporosis and uterine leiomyoma.
    Levonorgestrel
  • HY-18705
    Azoramide
    		Inhibitor 99.72%
    Azoramide is a potent, orally active small-molecule modulator of the unfolded protein response (UPR). Azoramide improves ER protein folding and elevates ER chaperone capacity, which together protects cells against ER stress. Azoramide alleviates PLA2G6 mutant-induced ER stress through modulating unfolded protein response, and enhances the CERB signaling to rescue mitochondrial function, thereby preventing apoptosis of DA neurons. Azoramide has antidiabetic activity.
    Azoramide
  • HY-13560
    AVN-944
    		Modulator 99.77%
    AVN-944 (VX-944) is an orally active, potent, selective, noncompetitive and specific inhibitor of IMPDH (inosine monophosphate dehydrogenase). AVN-944 is an essential rate-limiting enzyme in de novo guanine nucleotide synthesis. AVN-944 is also an inhibitor of arenavirus RNA synthesis, and blocks arenavirus infection. AVN-944 has broad anti-cancer activities, and can be used for multiple myeloma (MM) and acute myeloid leukemia (AML) research.
    AVN-944
  • HY-102027
    FX1
    		Inhibitor ≥98.0%
    FX1 is a potent and specific BCL6 inhibitor, with an IC50 of around 35 μM.
    FX1
  • HY-129179
    Lisaftoclax
    		Inhibitor 99.28%
    Lisaftoclax (compound 6) is a dual Bcl-2 and Bcl-xl inhibitor with anti-tumor activity, extracted from patent WO2018027097A1. Lisaftoclax exhibits IC50 values of 2 nM and 5.9 nM for Bcl-2 and Bcl-xl, respectively.
    Lisaftoclax
  • HY-N0213
    Peiminine
    		99.94%
    Peiminine is a compound that can be isolated from Bolbostemma paniculatum (Maxim) Franquet (Cucurbitaceae family). Peiminine can induce apoptosis in human hepatocellular carcinoma HepG2 cells through both extrinsic and intrinsic apoptotic pathways. Peiminine has anti-inflammatory, anticancer, anti-osteoporosis, cardioprotective and other activities in many animal models.
    Peiminine
  • HY-125877
    PROTAC Mcl1 degrader-1
    		Inhibitor 98.13%
    PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC) based on Cereblon ligand, is a potently and selectively Mcl-1 (Bcl-2 family member) inhibitor with an IC50 of 0.78 μM. PROTAC Mcl1 degrader-1 inhibits Bcl-2 with an IC50 of 0.54 μM.
    PROTAC Mcl1 degrader-1
  • HY-147081
    AS 1411
    		Inhibitor
    AS 1411 (AGRO-100) is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. AS 1411 works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. AS 1411-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity.
    AS 1411
  • HY-109185
    Pelcitoclax
    		Inhibitor 99.70%
    Pelcitoclax (APG-1252) is a potent Bcl-2/Bcl-xl inhibitor with antineoplastic and pro-apoptotic effects.
    Pelcitoclax
  • HY-126741
    Azadirachtin
    		Inhibitor 99.06%
    Azadirachtin is an oral active triterpenoid compound with anticancer, antimalarial, anti-inflammatory, and insecticidal activities. Azadirachtin induces cell apoptosis through the mitochondrial pathway (by inhibiting Bcl-2/Bax ratio or activating Apaf-1 and caspase-3) or through death receptors (by inhibiting TNFR activation). Additionally, Azadirachtin exerts its anti-inflammatory effects by inhibiting NF-кB signaling pathway activation, and it exhibits insecticidal activity by inducing apoptosis in insect cells.
    Azadirachtin
  • HY-N3584
    Paris saponin VII
    		Inhibitor 99.96%
    Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia.
    Paris saponin VII
  • HY-120079
    MSN-125
    		Inhibitor 99.00%
    MSN-125 is a potent Bax and Bak oligomerization inhibitor. MSN-125 prevents mitochondrial outer membrane permeabilization (MOMP) with an IC50 of 4 μM. MSN-125 potently inhibits Bax/Bak-mediated apoptosis in HCT-116, BMK Cells, and primary cortical neurons, protects primary neurons against glutamate excitotoxicity.
    MSN-125
  • HY-123054
    BTSA1
    		Activator 99.49%
    BTSA1 is a potent, high affinity and orally active BAX activator with an IC50 of 250 nM and an EC50 of 144 nM. BTSA1 binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis.
    BTSA1
  • HY-B0402A
    Amantadine hydrochloride
    		Modulator ≥98.0%
    Amantadine (1-Adamantanamine) hydrochloride is an orally avtive and potent antiviral agent with activity against influenza A viruses. Amantadine hydrochloride inhibits several ion channels such as NMDA and M2, and also inhibits Coronavirus ion channels. Amantadine hydrochloride also has anti-orthopoxvirus and anticancer activity. Amantadine hydrochloride can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research.
    Amantadine hydrochloride
  • HY-B0621
    Triclabendazole
    		98.72%
    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
  • HY-125876
    PROTAC Bcl2 degrader-1
    		Inhibitor 99.80%
    PROTAC Bcl2 degrader-1 (Compound C5) is a PROTAC based on Cereblon ligand, which potently and selectively induces the degradation of Bcl-2 (IC50, 4.94 μM; DC50, 3.0 μM) and Mcl-1 (IC50, 11.81 μM) by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1/Bcl-2 dual inhibitor Nap-1 (Blue: CRBN ligand, Black: linker；Pink: Mcl-1/Bcl-2 inhibitor, Nap-1).
    PROTAC Bcl2 degrader-1
  • HY-B0987
    Ascorbyl palmitate
    		Inhibitor 99.61%
    Ascorbyl palmitate is an orally active ester formed from ascorbic acid and palmitic acid, used as an antioxidant and food additive. Ascorbyl palmitate in preventing fat and oil oxidation is more efficient than Butylated hydroxyanisole (HY-B1066) and Butylated hydroxytoluene (HY-Y0172). Ascorbyl palmitate mitigates inhibition of collagen synthesis by select calcium and sodium channel blockers. Ascorbyl palmitate induces Apoptosis in human umbilical vein endothelial cells (HUVECs). Ascorbyl palmitate ameliorates inflammatory diseases by inhibition of NLRP3 inflammasome.
    Ascorbyl palmitate
  • HY-B0766
    Bicyclol
    		99.91%
    Bicyclol (SY801) is an orally active derivative of the traditional Chinese medicine Schisandra chinensis, which has antiviral, anti-inflammatory, immunomodulatory, antioxidant, anti-steatosis, anti-fibrotic and anti-tumor activities. Bicyclol regulates the expression of heat shock proteins and plays an anti-apoptosis role in hepatocytes. Bicyclol reduces the activation of NF-κB and the levels of inflammatory factors in hepatocytes infected with hepatitis C virus (HCV) by inhibiting the activation of the ROS-MAPK-NF-κB pathway, and prevents ferroptosis in acute liver injury. Bicyclol can change the expression of Mdr-1, GSH/GST and Bcl-2, increase the intracellular concentration of anticancer drugs, and sensitize drug-resistant cells to anticancer drugs. Bicyclol inhibits the proliferation of human malignant hepatoma cells by regulating the PI3K/AKT pathway and the Ras/Raf/MEK/ERK pathway. Bicyclol can be used in the study of chronic hepatitis, acute liver injury, nonalcoholic fatty liver disease, liver fibrosis and hepatocellular carcinoma.
    Bicyclol
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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