1046787-18-1

PKC-IN-1 is a potent, ATP-competitive and reversible inhibitor of conventional PKC enzymes with Kis of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively.

Human PKCα: 2.3 nM (IC₅₀); Human PKCβII: 7.6 nM (IC₅₀); Human PKCβI: 8.1 nM (IC₅₀); Human PKCθ: 25.6 nM (IC₅₀); Human PKCγ: 57.5 nM (IC₅₀); Human PKC mu: 314 nM (IC₅₀); Human PKCε: 808 nM (IC₅₀); Human PKCβ: 5.3 nM (Ki); Human PKCα: 10.4 nM (Ki)

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[1] Michael Niesman, et al. Treatment of autoimmune disease. WO2015179847A1.