apkc inhibitor

PHA-543613 hydrochloride acts as a potent and selective agonist for the α7 subtype of neural nicotinic acetylcholine receptors, with a high level of brain penetration and good oral bioavailability. It is under development as a possible treatment for cognitive deficits in schizophrenia.

PS315 inhibits the full-length and catalytic domain constructs of PKCζ (IC50=10 μM) and PKCη (IC50=30 μM). PS315 has anti-cancer activity. PS315 is a derivative of PS48 and is an allosteric PKC inhibitor by binding to the PIF-pocket of aPKC and inducing d

PKC-IN-4 (compound 7l) is a highly potent and orally active inhibitor of atypical protein kinase C (aPKC), with an IC 50 value of 0.52 µM. In vitro studies show that PKC-IN-4 effectively suppresses NF-κB activity induced by TNF-α and impedes retinal vasculature permeability induced by both VEGF and TNF-α. [1]

aPKC-I is an inhibitor of atypical protein kinase C (aPKC ) which inhibits both PKCζ and PKCι with high specificity and prevents VEGF-induced endothelial permeability in cell culture and in vivo, thereby blocking ischemia-reperfusion (IR)-induced permeability.