PKC beta II inhibitor H6

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PKC-IN-1 是一种有效的 PKC beta II 抑制剂，Ki 为 14.9 nM。

PKC-IN-1 is a poent PKC beta II inhibitor with Ki of 14.9 nM, extracted from patent WO 2008096260 A1 as compound example H6.

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.

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.

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Angiogenesis

PKC

PKC

Cancer

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1046787-18-1

500.623

C25H37FN8O2

>98% (HPLC)

DMSO : ≥ 25 mg/mL 49.94 mM

CC1CN(C(CN1C(=O)N2CC3=C(C2(C)C)NN=C3NC4=NC(=NC=C4F)C)C)CC5CCOCC5

((2S,5R)-2,5-dimethyl-4-((tetrahydro-2H-pyran-4-yl)methyl)piperazin-1-yl)(3-((5-fluoro-2-methylpyrimidin-4-yl)amino)-6,6-dimethyl-4,6-dihydropyrrolo[3,4-c]pyrazol-5(1H)-yl)methanone

(-20℃)

With Ice Pack

≥ 2 years