PKC beta II inhibitor H6( —— )

Catalog No. M10233 CAS No. 1046787-18-1

PKC-IN-1 is a poent PKC beta II inhibitor with Ki of 14.9 nM.

Purity : >98% (HPLC)

COA

Datasheet

HNMR

HPLC

MSDS

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Biological Information

Product Name

PKC beta II inhibitor H6
Note

Research use only, not for human use.
Brief Description

PKC-IN-1 is a poent PKC beta II inhibitor with Ki of 14.9 nM.
Description

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.
In Vitro

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.
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.
Synonyms

——
Pathway

Angiogenesis
Target

PKC
Recptor

PKC
Research Area

Cancer
Indication

——

Chemical Information

CAS Number

1046787-18-1
Formula Weight

500.623
Molecular Formula

C25H37FN8O2
Purity

>98% (HPLC)
Solubility

DMSO : ≥ 25 mg/mL 49.94 mM
SMILES

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

((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

Shipping & Storage Information

Storage

(-20℃)
Shipping

With Ice Pack
Stability

≥ 2 years

Reference

1. 3-Aminopyrrolo[3,4-c]pyrazole-5(1H,4H,6H)carboxaldehyde derivatives as PKC inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases. From PCT Int. Appl. (2008), WO 2008096260 A1 20080814.

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