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GKI-1

CAS No. 2444764-03-6

GKI-1( —— )

Catalog No. M32936 CAS No. 2444764-03-6

GKI-1 is a Greatwall (GWL) kinase inhibitor with an IC50 of 4.9 for hGWLFL and 2.5 μM for hGWL-KinDom. It exhibits stronger inhibition on ROCK1 with an IC50 of 11 μM and only weakly inhibits PKA.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    GKI-1
  • Note
    Research use only, not for human use.
  • Brief Description
    GKI-1 is a Greatwall (GWL) kinase inhibitor with an IC50 of 4.9 for hGWLFL and 2.5 μM for hGWL-KinDom. It exhibits stronger inhibition on ROCK1 with an IC50 of 11 μM and only weakly inhibits PKA.
  • Description
    GKI-1 is a Greatwall (GWL) kinase inhibitor with IC50s of 4.9 and 2.5 μM against hGWLFL and hGWL-KinDom, respectively. GKI-1 robustly inhibits ROCK1 with an IC50 of 11 μM, but only weakly affected PKA.
  • In Vitro
    GKI-1 inhibits full-length human GWL, and shows cellular efficacy. Treatment of HeLa cells (25 and 50 μM, 0-8.5 hours) with GKI-1 reduces ENSA/ARPP19 phosphorylation levels, resulting in a decrease in mitotic events, mitotic arrest/cell death and cytokinesis failure.
  • In Vivo
    ——
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    Others
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2444764-03-6
  • Formula Weight
    269.73
  • Molecular Formula
    C15H12ClN3
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 200 mg/mL (741.48 mM; Ultrasonic )
  • SMILES
    N(C=1C=C(C=CC1)C=2C=NNC2)C3=CC=C(Cl)C=C3
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Ocasio CA, et al. A first generation inhibitor of human Greatwall kinase, enabled by structural and functional characterisation of a minimal kinase domain construct. Oncotarget. 2016 Nov 1;7(44):71182-71197.?
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