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-118948
    MSN-50
    		Inhibitor 98.68%
    MSN-50 is a Bax and Bak oligomerization inhibitor. MSN-50 efficiently inhibits liposome permeabilization, prevents genotoxic cell death and promotes neuroprotection.
    MSN-50
  • HY-N1939
    Icariside I
    		99.30%
    Icariside I (GH01) is an orally active metabolite of icalin. Icariside I improves estrogen deficiency-induced osteoporosis by simultaneously regulating osteoblast and osteoclast differentiation. Icariside I promotes ATP (HY-B2176) or Nigericin (HY-127019)-induced mtROS production and NLRP3 inflammasome activation and causes idiosyncratic hepatotoxicity. Icariside I does not alter the activation of NLRC4 and AIM2 inflammasomes. Icariside I inhibits breast cancer proliferation, apoptosis, invasion, and metastasis by targeting the IL-6/STAT3 pathway. Icariside I is a kynurenine-AhR pathway inhibitor that alleviates cancer by blocking tumor immune escape.
    Icariside I
  • HY-113438
    15(S)-HPETE
    		Inhibitor
    15(S)-HPETE is a precursor of 15(S)-HETE (HY-113336). 15(S)-HPETE is a product of Arachidonic acid (HY-109590) in the 15-lipoxygenase pathway. 15(S)-HPETE reduces Bcl-2, Akt, and phosphorylated Akt protein levels. 15(S)-HPETE induces Apoptosis. 15(S)-HPETE antagonizes the angiogenic effects of 15(S)-HETE. 15(S)-HPETE exhibits antitumor effects against chronic myeloid leukemia. 15(S)-HPETE can be used in adipose tissue explant studies.
    15(S)-HPETE
  • HY-Y0396
    N-Hydroxyphthalimide
    		Inhibitor 99.89%
    N-Hydroxyphthalimide is a blocking agent and catalyst. N-Hydroxyphthalimide promotes oxidation reactions by generating PINO free radicals and activating hydrogen atom transfer processes. N-Hydroxyphthalimide reduces the expression of anti-apoptotic proteins Survivin and Bcl-xL and activates caspase 9 and caspase 3. N-Hydroxyphthalimide induces Apoptosis. N-Hydroxyphthalimide inhibits the phosphorylation of mTOR (Ser2448, Ser2481) and Akt (Ser473). N-Hydroxyphthalimide has anticancer effects against breast and colon cancer.
    N-Hydroxyphthalimide
  • HY-13108
    Bz 423
    		Activator 99.72%
    Bz 423 is a pro-apoptotic 1,4-benzodiazepine with therapeutic properties in murine models of lupus demonstrating selectivity for autoreactive lymphocytes, and activates Bax and Bak.
    Bz 423
  • HY-117288
    S55746
    		Inhibitor 99.91%
    S55746 (BCL201) is a potent, orally active and selective BCL-2 inhibitor, with a Ki of 1.3 nM and a Kd of 3.9 nM. S55746 (BCL201) has antitumor activity with low toxicity.
    S55746
  • HY-W082785A
    L6H21
    		Modulator 99.19%
    L6H21, a Chalcone (HY-121054) derivative, is an orally active, potent and specific myeloid differentiation 2 (MD-2) inhibitor. L6H21 directly binds to MD-2 protein with a high affinity and low KD value of 33.3 μM, blocking the formation of the LPS-TLR4/MD-2 complex. L6H21 inhibits LPS-induced expression of TNF-α and IL-6 in RAW264.7 macrophages, with IC50 values of 6.58 and 8.59 μM, respectively. L6H21 can be used for alcoholic liver disease, metabolic disturbance and neuroinflammation research.
    L6H21
  • HY-B1839
    Fluazinam
    		Inhibitor 99.36%
    Fluazinam is an orally active dinitroaniline fungicide. Fluazinam induces phosphorylation of JNK, activates p38 pathway, decreases Bcl-2, activates caspase-3, decreases complex I activity, increases Autophagy and Apoptosis. Fluazinam has strong antifungal activity against F. fujikuroi and B. maydis. Fluazinam has a negative impact on Brachydanio rerio and worker bees.
    Fluazinam
  • HY-15464
    (R)-(-)-Gossypol
    		Inhibitor 98.82%
    (R)-(-)-Gossypol (AT-101) is the levorotatory isomer of a natural product Gossypol. AT-101 is determined to bind to Bcl-2, Mcl-1 and Bcl-xL proteins with Kis of 260±30 nM, 170±10 nM, and 480±40 nM, respectively.
    (R)-(-)-Gossypol
  • HY-146185
    CCT373566
    		Inhibitor 99.61%
    CCT373566 is a potent and orally active molecular glue degrader of transcriptional repressor BCL6, with an IC50 of 2.2 nM. CCT373566 shows strong antiproliferative efficacy in vitro and reduction in tumor growth in vivo.
    CCT373566
  • HY-121705
    Propionyl-L-carnitine
    Propionyl-L-carnitine is an orally active L-carnitine derivative. Propionyl-L-carnitine has a high affinity for muscle L-carnitine transferase. Propionyl-L-carnitine increases Apoptosis, Bax, and reduces NF-κB, VCAM-1, MCP-1, and survivin. Propionyl-L-carnitine activates Src kinase, Akt, induces p-AMPK and nitric oxide synthesis. Propionyl-L-carnitine alleviates cardiovascular disease, obesity, and colitis.
    Propionyl-L-carnitine
  • HY-115930
    Bim-IN-1
    		Inhibitor 99.57%
    Bim-IN-1 is a potent Bim expression inhibitor. Bim-IN-1 reduces Bim expression levels and has little inhibitory effect upon protein kinase A activity and minimal toxicity.
    Bim-IN-1
  • HY-101259
    BMS-195614
    		99.5%
    BMS-195614 (BMS 614) is an orally active neutral RARα-selective antagonist with a Ki of 2.5 nM. BMS-195614 restores the expression of Bcl2. BMS-195614 inhibits the transactivation of NF-κB, AP-1 and PPAR. BMS-195614 downregulates the expression of IL-6 and VEGF. BMS-195614 reduces blue light-induced phototoxicity and inhibits cell migration. BMS-195614 modulates inflammation and angiogenesis.
    BMS-195614
  • HY-W042191
    Oxychlororaphine
    		Modulator 98.98%
    Oxychloroaphine could be isolated from the bacterium Pantoea agglomerans naturally present in soil. Oxychloroaphine has broad-spectrum antifungal activity. Oxychloroaphine has cytotoxicity in a dose-dependent manner and induces apoptosis. Oxychloroaphine can be used in research of cancer.
    Oxychlororaphine
  • HY-12020
    TW-37
    		Inhibitor 99.50%
    TW-37 is a potent Bcl-2 inhibitor with Ki values of 260, 290 and 1110 nM for Mcl-1, Bcl-2 and Bcl-xL, respectively.
    TW-37
  • HY-N2575
    Hypocrellin A
    		99.73%
    Hypocrellin A is a PKC inhibitor that exerts antidiabetic activity by reversing the effects of high glucose on endothelin (ET-1) expression. Hypocrellin A is also a photosensitizer for photodynamic therapy (PDT) with anticancer, antibacterial and antiviral activities, especially against human immunodeficiency virus (HIV). In addition, Hypocrellin-A also possesses anti-Leishmania activity (IC50=0.27 μg/ml).
    Hypocrellin A
  • HY-W016412
    Coenzyme Q0
    		Modulator 99.79%
    Coenzyme Q0 (CoQ0) is a potent, oral active ubiquinone compound can be derived from Antrodia cinnamomea. Coenzyme Q0 induces apoptosis and autophagy, suppresses of HER-2/AKT/mTOR signaling to potentiate the apoptosis and autophagy mechanisms. Coenzyme Q0 regulates NFκB/AP-1 activation and enhances Nrf2 stabilization in attenuation of inflammation and redox imbalance. Coenzyme Q0 has anti-angiogenic activity through downregulation of MMP-9/NF-κB and upregulation of HO-1 signaling.
    Coenzyme Q0
  • HY-44432
    Navitoclax-piperazine
    		Inhibitor 99.73%
    Navitoclax-piperazine (ABT-263-piperazine) is a Navitoclax (HY-10087) analog and BCL-XL inhibitor. Navitoclax-piperazine is the ligand for target protein of PROTAC DT2216 (HY-130604). Navitodax-pperaie and E3 ubiquitin ligase VHL ligand can be used to synthesize PROTAC DT2216 (HY-130604).
    Navitoclax-piperazine
  • HY-112859
    VU0661013
    		Inhibitor 98.45%
    VU661013 is a potent and selective MCL-1 inhibitor.
    VU0661013
  • HY-126437
    Poly-L-lysine hydrobromide (MW 30000-70000)
    		Inhibitor
    Poly-L-lysine hydrobromide (MW 30000-70000) is a water-soluble synthetic polypeptide. Poly-L-lysine hydrobromide (MW 30000-70000) downregulates Bcl-2 and upregulates Bax and p53 proteins. Poly-L-lysine hydrobromide (MW 30000-70000) promotes Apoptosis and reduces VEGF expression. Poly-L-lysine hydrobromide (MW 30000-70000) shows anticancer activity against a variety of tumors. Poly-L-lysine hydrobromide (MW 30000-70000) can also be used as a coating material.
    Poly-L-lysine hydrobromide (MW 30000-70000)
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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