PKC-IN-1 是ATP-竞争性可逆PKC抑制剂，对人 PKCβ 和 PKCα 的Ki值分别为 5.3 和 10.4 nM，对人 PKCα、PKCβI、PKCβII、PKCθ、PKCγ、PKC mu 和 PKCε 的IC50值分别为 2.3、8.1、7.6、25.6、57.5、314 和 808 nM。

PKC-IN-1 is an ATP-competitive and reversible conventional PKC enzymes inhibitor (PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε with IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM, respectively).

PKC-IN-1 is a potent, ATP-competitive, and reversible of conventional PKC enzymes (PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε 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, respectively) [1].

In Lewis rats, PKC-IN-1 dose-dependently and significantly reduces maximum EAE severity and end severity in the autoimmune encephalitis (EAE) model [1].

1046787-18-1

C25H37FN8O2

500.61

DMSO:25 mg/mL (49.94 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years