Table 2.

Representative PKC Inhibitors.

Chemical Group	Example	Site of Action	Specificity
1-(5-isoquinolinesulfonyl)-2-methylpiperazines	H-7	Catalytic domain Compete with ATP at the ATP binding site	Also, inhibits cyclic AMP and cyclic GMP-dependent protein kinases
Microbial Alkaloids, Products of Streptomyces	Staurosporine SCH47112	Catalytic domain, ATP binding site	Also, inhibits MLC kinase and tyrosine kinase
Benzophenanthridine Alkaloids	Chelerythrine	Catalytic domain	Competitive inhibitor with histone IIIS
Indocarbazoles	Gö6976	Catalytic domain	Ca2+-dependent α- and βI-PKC
Bisindolylmaleimide Staurosporine Analogs	GF109203X Ro-318220 Midostaurin (PKC412, CGP41251) Ruboxistaurin (LY333531)	Catalytic domain	PKC isozymes α, βI, βII, γ, δ and ε. Ruboxistaurin mesylate is a selective antagonist of PKC βI and PKC βII.
Perylenequinone Metabolites from Cladosporium cladosporioides	Calphostin C (UCN-1028A)	Regulatory domain	Binds to the regulatory domain at DAG/phorbol ester binding site
Membrane lipids	Sphingosine	Regulatory domain	Competitive inhibitor with phosphatidylserine
Other:	Adriamycin Aminoacridine Apigenin Cercosporin Chlorpromazine Dexniguldipine Polymixin B Sangivamycin Tamoxifen Trifluoperazine UCN-01, UCN-02