Chemical Properties
Dark red solid
Uses
Potent inhibitor of protein kinase C
Uses
Calphostin C (PKF115-584) is a perylenequinione isolated from the fungus, Cladosporium cladosporioides. Calphostin C is a potent and specific inhibitor of protein kinase C (PKC), with inhibition being light dependent. Calphostin C inhibits cell proliferation and induces apoptosis in vitro. Calphostin C is an antagonist of Tcf4/b-catenin signalling, inhibiting the expression of survivin and inducing apoptosis in several tumor cell lines.
Uses
Calphostin C (CGP049090) is a perylenequinione isolated from the fungus, Cladosporium cladosporioides. Calphostin C is a potent and specific inhibitor of protein kinase C (PKC), with inhibition being light dependent. Calphostin C inhibits cell proliferation and induces apoptosis in vitro. Calphostin C is an antagonist of Tcf4/b-catenin signalling, inhibiting the expression of survivin and inducing apoptosis in several tumour cell lines.
Biological Activity
Potent, selective and photo-dependent inhibitor of protein kinase C that targets the regulatory domain (IC 50 = 50 nM). Displays > 1000-fold selectivity over other protein kinases such as cAMP-dependent protein kinase and tyrosine-specific protein kinase. Inhibits cell proliferation of malignant glioma cells in light-treated conditions in vitro (IC 50 ~ 40-60 nM).
Biochem/physiol Actions
Highly specific inhibitor of protein kinase C (IC50 = 50 nM); requires light for activation. At higher concentrations (100 nM or greater), it has been shown to inhibit cell proliferation and induce apoptosis in vitro.
