Bryostatin 1 (NSC 339555) is a macrocyclic lactone derived from a marine invertebrate, fuctions as an activator of PKC with high binding affinity (Ki=1.35 nM).

Safingol hydrochloride (L-threo-dihydrosphingosine hydrochloride) is a specific inhibitor of protein kinase C. It induces autophagy in solid tumor cells and cancer cell death by inhibiting the PKC and PI3-kinase pathways.

Fumagillin is a selective and potent irreversible inhibitor of Methionine aminopeptidase 2 (MetAP2), used as an antibiotic to treat microsporidiosis.