1160501-81-4

PKC-theta inhibitor 1 is the PKCθ inhibitor with an Ki value of 6 nM, inhibits IL-2 production in vivo with an IC50 of 0.19 μM. PKC-theta inhibitor 1 demonstrates a reduction of symptoms in a mouse model of multiple sclerosis[1].

PKCθ: 6 nM (Ki); PKCδ: 392 μM (Ki); PKCα: 1020 μM (Ki); IL-2 production: 0.19 μM (IC₅₀)

[1] Collier PN, et al. Discovery of Selective, Orally Bioavailable Pyrazolopyridine Inhibitors of Protein Kinase Cθ (PKCθ) That Ameliorate Symptoms of Experimental Autoimmune Encephalomyelitis. ACS Med Chem Lett. 2019 Jun 27;10(8):1134-1139. DOI:10.1021/acsmedchemlett.9b00134