產品描述: | 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. |
靶點: |
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);PKC |
體外研究: |
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 |
體內研究: |
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 |
參考文獻: |
1. Michael Niesman, et al. Treatment of autoimmune disease. WO2015179847A1. |
溶解性: |
soluble in DMSO |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
1.998 ml |
9.988 ml |
19.976 ml |
5 mM |
0.4 ml |
1.998 ml |
3.995 ml |
10 mM |
0.2 ml |
0.999 ml |
1.998 ml |
50 mM |
0.04 ml |
0.2 ml |
0.4 ml |
|
注意: |
部分產品我司僅能提供部分信息,我司不保證所提供信息的權威性,僅供客戶參考交流研究之用。 |