CALPHOSTIN C

Chemical properties

Dark red solid

The Uses of CALPHOSTIN C

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.

The Uses of CALPHOSTIN C

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.

The Uses of CALPHOSTIN C

Potent inhibitor of protein kinase C

What are the applications of Application

Calphostin C is an inhibitor of PKC, PKA, PKG, and calcium channel proteins

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.

Storage

+4°C (desiccate)