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GKI-1 

Cat. No.: HY-100521
Handling Instructions

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.

For research use only. We do not sell to patients.

GKI-1 Chemical Structure

GKI-1 Chemical Structure

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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[1].

IC50 & Target

IC50: 4.9 µM (hGWLFL), 4.9 µM (hGWL-KinDom)[1]

In Vitro

GKI-1 inhibits full-length human GWL, and shows cellular efficacy[1].

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[1].

Molecular Weight

269.73

Formula

C₁₅H₁₂ClN₃

SMILES

ClC(C=C1)=CC=C1NC2=CC(C3=CNN=C3)=CC=C2

Shipping

Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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GKI-1
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HY-100521
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