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-132173
    GL0388
    		Activator 98.03%
    GL0388 is a Bax activator that results in Bax insertion into mitochondrial membrane. GL0388 shows antiproliferative activities against various cancer cells, with IC50s of 0.299-1.57 μM. GL0388 activates Bax and induce Bax-mediated apoptosis. GL0388 suppresses breast cancer xenograft tumor growth in vivo.
    GL0388
  • HY-128360
    dMCL1-2
    		Degrader 99.29%
    dMCL1-2 is a potent, selective MCL1 PROTAC degrader based on a Cereblon ligand, with a KD value of 30 nM for binding to MCL1. dMCL1-2 induces ubiquitination and degradation of MCL1. dMCL1-2 degrades MCL1, cleaves Caspase-3, and induces Apoptosis. dMCL1-2 can be used in research related to multiple myeloma.
    dMCL1-2
  • HY-16967
    MM41
    		Inhibitor 98.89%
    MM41 is a quadruplex-interacting compound. MM41 binds tightly to quadruplexes encoded in the promoter sequences of the BCL-2 and k-RAS genes. MM41 reduces BCL-2 and k-RAS protein levels, increases caspase 3. MM41 has antitumor effects against pancreatic cancer.
    MM41
  • HY-132307
    Mcl-1 inhibitor 6
    		Inhibitor 98.77%
    Mcl-1 inhibitor 6 is an orally active, selective myeloid cell leukemia 1 (Mcl-1) protein inhibitor with a Kd of 0.23 nM and a Ki of 0.02 μM. Mcl-1 inhibitor 6 possesses superior selectivity over other Bcl-2 family members (Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w, Kd>10 μM). Mcl-1 inhibitor 6 is a potent antitumor agent.
    Mcl-1 inhibitor 6
  • HY-155472
    Mcl-1 inhibitor 17
    		Inhibitor 99.41%
    Mcl-1 inhibitor 17 is a Mcl-1 protein inhibitor. Mcl-1 inhibitor 17 can be used for the research of cancer and other diseases.
    Mcl-1 inhibitor 17
  • HY-169265
    BRD-K20733377
    		Inhibitor 99.50%
    BRD-K20733377 is an inhibitor for Bcl-2, and exhibits selective cytotoxicity against senescent cells, that inhibits the viability of Etoposide (HY-13629)-induced IMR-90 senescent cell with an IC50 of 10.7 μM. BRD-K20733377 reduces the mRNA expression of aging-related genes p16, p21 and KI67 in aged mouse model.
    BRD-K20733377
  • HY-131232
    Desmorpholinyl Navitoclax-NH-Me
    		Inhibitor 98.64%
    Desmorpholinyl Navitoclax-NH-Me is a Bcl-xL inhibitor. Desmorpholinyl Navitoclax-NH-Me and a CRBN ligand for the E3 ubiquitin ligase can be used in the synthesis of PROTAC BCL-XL degrader XZ739 (HY-133557).
    Desmorpholinyl Navitoclax-NH-Me
  • HY-16942
    Damulin B
    		Inhibitor
    Damulin B is a dammarane-type saponin found in Gynostemma pentaphyllum. Damulin B can inhibit cancer cell apoptosis, decrease mitochondrial membrane potential, inhibit ROS production and cause G0/G1 phase arrest. Damulin B can prevent Cisplatin (HY-17394)-induced acute kidney injury and induce hair growth. Damulin B shows anti-inflammation anti-diabetic and anti-obesity effect. Damulin B can be used for the researches of cancer, inflammation, metabolic disease, such as lung cancer, osteoarthritis and diabetes.
    Damulin B
  • HY-114118S1
    Semaglutide-d8 tetraTFA
    		99.87%
    Semaglutide-d8 tetraTFA is the deuterium labeled Semaglutide (HY-114118). Semaglutide is a long-acting, selective, competitive GLP-1R agonist that can penetrate the blood-brain barrier. After activating GLP-1R, Semaglutide promotes insulin secretion, inhibits gastric emptying and appetite, and at the same time enhances autophagy, inhibits oxidative stress and apoptosis. Semaglutide also regulates mitochondrial function and lipid metabolism (such as reducing de novo lipogenesis in the liver). Semaglutide 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 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-d<sub>8</sub> tetraTFA
  • HY-101083
    BDA-366
    		Antagonist 98.42%
    BDA-366 is a potent Bcl2 antagonist (Ki = 3.3 nM), binding Bcl2-BH4 domain with high affinity and selectivity. BDA-366 induces conformational change in Bcl2 that abrogates its antiapoptotic function, converting it from a survival molecule to a cell death inducer. BDA-366 suppresses growth of lung cancer cells.
    BDA-366
  • HY-147929
    Apoptotic agent-3
    		Activator 98.19%
    Apoptotic agent-3 (compound 15f) promotes apoptosis through the potential mitochondria-mediated Bcl-2/Bax pathway and activation of the Caspase 3 pathway. Apoptotic agent-3 exhibits anti-proliferative activities and can be used for cancer research.
    Apoptotic agent-3
  • HY-N3001
    Isolinderalactone
    		Inhibitor 98.79%
    Isolinderalactone is a sesquiterpene that exhibits anti-cancer, anti-inflammatory, and neuroprotective effects. Isolinderalactone inhibits VEGF expression and tyrosine phosphorylation of VEGFR2. Isolinderalactone decreases viability and induces apoptosis in U-87 glioblastoma (GBM) cells and colorectal cancer (CRC) cells. Isolinderalactone induces G2/M phase cell cycle arrest, ROS generation, pJNK/p38 MAPK activation, in colorectal cancer (CRC) cells. Isolinderalactone blocks LPS (HY-D1056)-induced NF-κB activation while activating Nrf2-HMOX1 signaling in RAW264.7 macrophages. Isolinderalactone improves cognitive dysfunction in APP/PS1 mice. Isolinderalactone can be used for the study of Glioblastoma multiforme (GBM), colorectal cancer, Alzheimer’s disease and acute lung injury.
    Isolinderalactone
  • HY-N1157
    Thevetiaflavone
    		Modulator 99.83%
    Thevetiaflavone could upregulate the expression of Bcl-2 and downregulate that of Bax and caspase-3.
    Thevetiaflavone
  • HY-15613
    Maritoclax
    		Inhibitor 99.97%
    Maritoclax (Marinopyrrole A) is a novel and specific Mcl-1 inhibitor with an IC50 value of 10.1 μM, and shows >8 fold selectivity than BCL-xl (IC50 > 80 μM).
    Maritoclax
  • HY-111954
    (+)-Erinacin A
    		99.81%
    (+)-Erinacin A (Erinacine A) is a cyanoditerpenoid isolated from Hericium erinaceus with anticancer, anti-inflammatory and neuroprotective activities. (+)-Erinacin A can induce cancer cell death by activating extrinsic and intrinsic apoptosis pathways. (+)-Erinacin A can also inhibit the expression of NO synthase (iNOS) and the production of nitrotyrosine to exert inflammatory and neuroprotective effects, thereby reducing ischemic brain damage.
    (+)-Erinacin A
  • HY-N2115
    Araloside A
    		Inhibitor 99.86%
    Araloside A (Chikusetsusaponin IV), triterpenoid saponins, is an orally active component of Aralia elata. Araloside A shows low-renin-inhibitory activity with an IC50 of 77.4 μM. Araloside A can inhibit cell proliferation and induce apoptosis. Araloside A suppresses inflammatory cytokines IL-1β and IL-6 production. Araloside A can be used for the researches of cancer, inflammation and cardiovascular disease, such as renal cell carcinoma and rheumatoid arthritis.
    Araloside A
  • HY-158783
    SACLAC
    		Activator 99.70%
    SACLAC, a Ceramide analog, is a potent and covalent acid ceramidase (ASAH1; AC) inhibitor with a Ki of 97.1 nM. SACLAC effectively blocks AC activity and induces a decrease in sphingosine 1-phosphate (S1P) and total ceramide levels. SACLAC reduces the levels of splicing factor SF3B1 and alternative Mcl-1 mRNA splicing, increases pro-apoptotic Mcl-1S levels to induce apoptosis in acute myeloid leukemia (AML) cells. SACLAC reduces the leukemic burden in human AML xenograft mouse models.
    SACLAC
  • 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-167881
    MLS-0053105
    		Inhibitor 98.89%
    MLS-0053105, a chloromaleimide, is a selective BFL-1 inhibitor with an IC50 of 0.4 µM for Bfl-1/F-Bid. MLS-0053105 shows over 10 times less potent inhibition of Bcl-W, Bcl-2, and Bcl-XL and no activity against Bcl-B and Mcl-1.
    MLS-0053105
  • HY-12286
    PI-1840
    		Modulator 98.78%
    PI-1840 is a potent and selective chymotrypsin-like (CT-L) inhibitor for with an IC50 value of 27 nM. PI-1840 inhibits cell proliferation and arrest cell cycle at G2/M phase. PI-1840 induces apoptosis and induces autophagy. PI-1840 induces the accumulation of proteasome substrates p27, Bax, and IκB-α.
    PI-1840
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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