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Chelerythrine chloride

An Inhibitor of Protein Kinase C, SERCA Pump, and P2X7 Receptor

Cat #: C-400
Lyophilized Powder yes
  • Bioassay Tested
    • Origin Macleaya Cordata.
    Source Natural
    MW: 383.84
    Purity: >99%
    Effective concentration 1-5 µM.
    Structure
    Chemical name 1,2-Dimethoxy-12-methyl[1,3]benzodioxolo[5,6-c]phenanthridinium chloride.
    Molecular formula C21H18ClNO4.
    CAS No.: 3895-92-9
    Activity Chelerythrine chloride is a potent, cell-permeable inhibitor of protein kinase C (PKC). It is at least 100-fold more selective for PKCs than for other kinases1,2.
    References-Activity
    1. Herbert, J.M. et al. (1990) Biochem. Biophys. Res. Commun. 172, 993.
    2. Chao, M.D. et al. (1998) Planta Med. 64, 662.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility Water or DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to two weeks at 4°C or six months at -20°C.
    Our bioassay
    • Alomone Labs Chelerythrine chloride inhibits NGF-mediated survival of serum-deprived PC12 cells.
      Alomone Labs Chelerythrine chloride inhibits NGF-mediated survival of serum-deprived PC12 cells.
      Dose-response curve of Chelerythrine chloride (#C-400) inhibition of the 100 ng/ml Native mouse NGF 2.5S protein (>95%) (#N-100) mediated survival of serum-deprived PC12 cells. IC50 was determined at 8.3 µM.
    • Alomone Labs Chelerythrine chloride inhibits PKC in NIH-3T3 cells.
      Alomone Labs Chelerythrine chloride inhibits PKC in NIH-3T3 cells.
      Cells were incubated with different concentrations of Chelerythrine chloride (#C-400) for 30 min and then stimulated with PMA (#P-800), (3 ng/ml) for 20 min. Cell proteins were resolved by SDS-PAGE and probed with anti-phospho (ser)-MARCKS (myristoylated alanin-rich protein kinase C substrate).
    References - Scientific background
    1. Herbert, J.M. et al. (1990) Biochem. Biophys. Res. Commun. 172, 993.
    2. Chao, M.D. et al. (1998) Planta Med. 64, 662.
    3. Ko, F.N. et al. (1990) Biochim. Biophys. Acta 1052, 360.
    4. Le Corvoisier, P. et al. (2002) Fundam. Clin. Pharmacol. 16, 31.
    5. Shi, L. and Wang, Ca. (1999) Arch. Biochem. Biophys. 368, 40.
    6. Sweeney, J.F. et al. (2000) Shock 13, 464.
    7. Chan, S.L. et al. (2003) J Biol. Chem. 278, 20453.
    8. Vieira, S.M. et al. (2015) Arch. Biochem. Biophys. 570, 58.
    9. Shemon, A.N. et al. (2004) Br. J. Pharmacol. 142, 1015.
    Scientific background

    Chelerythrine is a potent, cell-permeable inhibitor of protein kinase C (IC50 = 660 nM) that binds to the catalytic domain of PKC. Chelerythrine is at least 100-fold more selective for PKCs than for other kinases.1,2

    In platelets, Chelerythrine inhibits thromboxane formation and phosphoinositide metabolism.3,4 It has an inhibitory effect on ACh-induced current in PC12 cells.5

    Chelerythrine induces apoptotic cell death in polymorphonuclear leukocyte through activation of caspase-3.6 Furthermore, Chelerythrine treated cells underwent apoptosis, with features that suggest involvement of the mitochondrial pathway, and through a mechanism that involves inhibition of the anti-apoptotic inhibitor BclXL.7

    Chelerythrine inhibits SERCA pumps with an IC50 of 1.5 µM8. It also antagonizes P2X7 receptors; it inhibits ATP-induced 86Rb+ efflux with an IC50 of 5.6 µM9.

    Target PKC, SERCA pumps, P2X7 receptor
    Lyophilized Powder
    Last update: 13/10/2022

    Chelerythrine chloride (#C-400) is a highly pure, natural, and biologically active compound.

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    For research purposes only, not for human use
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