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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
Size Price / USD Stock Quantity
1 mL x 10 mM in DMSO 226 In Stock
5MG 212 In Stock
10MG 316 In Stock
25MG 511 In Stock
50MG 681 In Stock
100MG 921 In Stock
200MG Get Quote In Stock
500MG Get Quote In Stock
1G Get Quote In Stock
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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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