PKC-IN-1 |
| カタログ番号GC31711 |
PKC-IN-1 は、従来の PKC 酵素の強力な ATP 競合性および可逆的阻害剤であり、Kis はヒト PKCβ および PKCα に対して 5.3 および 10.4 nM であり、IC50 はヒト PKCβ および PKCα に対して 2.3、8.1、7.6、25.6、57.5、314、808 nM です。それぞれＰＫＣα、ＰＫＣβＩ、ＰＫＣβＩＩ、ＰＫＣθ、ＰＫＣγ、ＰＫＣミューおよびＰＫＣε。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1046787-18-1
Sample solution is provided at 25 µL, 10mM.
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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.
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