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。
产品描述
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).
体外活性
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].
体内活性
In Lewis rats, PKC-IN-1 dose-dependently and significantly reduces maximum EAE severity and end severity in the autoimmune encephalitis (EAE) model [1].
Cas No.
1046787-18-1
分子式
C25H37FN8O2
分子量
500.61
储存和溶解度
DMSO:25 mg/mL (49.94 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years