PKC-IN-1是一种有效的，ATP-竞争性的，可逆的PKC抑制剂，对人PKCβ和PKCα的Ki值分别为5.3和10.4nM，对人PKCα，PKCβI，PKCβII，PKCθ，PKCγ，PKCmu和PKCε的IC50值分别为2.3，8.1，7.6，25.6，57.5，314，808nM。
CAS：1046787-18-1
分子式：C25H37FN8O2
分子量：500.61
纯度：98%
存储：Store at -20°C

Background:

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.

PKC-IN-1 (Compound A) is a potent, ATP-competitive and reversible 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[1].

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[1].

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