Overview
- Herbert, J.M. et al. (1990) Biochem. Biophys. Res. Commun. 172, 993.
- Chao, M.D. et al. (1998) Planta Med. 64, 662.
- 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.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).
- Herbert, J.M. et al. (1990) Biochem. Biophys. Res. Commun. 172, 993.
- Chao, M.D. et al. (1998) Planta Med. 64, 662.
- Ko, F.N. et al. (1990) Biochim. Biophys. Acta 1052, 360.
- Le Corvoisier, P. et al. (2002) Fundam. Clin. Pharmacol. 16, 31.
- Shi, L. and Wang, Ca. (1999) Arch. Biochem. Biophys. 368, 40.
- Sweeney, J.F. et al. (2000) Shock 13, 464.
- Chan, S.L. et al. (2003) J Biol. Chem. 278, 20453.
- Vieira, S.M. et al. (2015) Arch. Biochem. Biophys. 570, 58.
- Shemon, A.N. et al. (2004) Br. J. Pharmacol. 142, 1015.
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.
Chelerythrine chloride (#C-400) is a highly pure, natural, and biologically active compound.
Applications
Citations
- Libster, A.M. et al. (2015) J. Neurophysiol. 114, 3339.
- De Chiara, V. et al. (2013) Neuroscience 250, 232.