| Bioactivity | 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. | ||||||||||||
| Invitro | 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]. | ||||||||||||
| In Vivo | 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]. | ||||||||||||
| Name | PKC-IN-1 | ||||||||||||
| CAS | 1046787-18-1 | ||||||||||||
| Formula | C25H37FN8O2 | ||||||||||||
| Molar Mass | 500.61 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [1]. Michael Niesman, et al. Treatment of autoimmune disease. WO2015179847A1. |
PKC-IN-1
CAS: 1046787-18-1 F: C25H37FN8O2 W: 500.61
PKC-IN-1 is a potent, ATP-competitive and reversible inhibitor of conventional PKC enzymes with Kis of 5.3 and 10.4 nM f
Sales Email：peptidedb@qq.com
This product is for research use only, not for human use. We do not sell to patients.