PKC-IN-1

PKC-IN-1 is a potent, ATP-competitive and reversible inhibitor of conventional PKC enzymes with K i s of 5.3 and 10.4 nM for human PKCβ and PKCα , and IC 50 s 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. In Vitro PKC-IN-1 (Compound A) is a potent, ATP-competitive and reversible of conventional PKC enzymes with K i s of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC 50 s 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo PKC-IN-1 (Compound A; 15 and 30 mg/kg, p.o., bid (twice a day)) dose-dependently and significantly reduces maximum EAE severity and end severity in autoimmune encephalitis (EAE) model in Lewis rats . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 2.3 nM (Human PKCα), 7.6 nM (Human PKCβII), 8.1 nM (Human PKCβI), 25.6 nM (Human PKCθ), 57.5 nM (Human PKCγ), 314 nM (Human PKC mu), 808 nM (Human PKCε), Ki: 5.3 nM (Human PKCβ), 10.4 nM (Human PKCα)

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