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).
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.
