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]

PKC:0.52 μM

PKC-IN-4 (compound 7l) demonstrates VEGF-induced endothelial permeability with an EC50 of 0.071 μM [1].

PKC-IN-4, administered at doses of 10 mg/kg intravenously (i.v.) and 20 mg/kg orally (p.o.), demonstrates oral activity with an oral bioavailability of 81.7% in CD-1 mice. This compound, when tested, exhibited favorable pharmacokinetic (PK) parameters, substantiating its effectiveness and potential for further development.