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PKC beta II inhibitor H6

CAS No. 1046787-18-1

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)

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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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