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GKI-1

Katalog-Nr.GC34381

GKI-1 ist ein Greatwall (GWL)-Kinase-Inhibitor mit IC50-Werten von 4,9 und 2,5 μM gegen hGWLFL bzw. hGWL-KinDom. GKI-1 hemmt ROCK1 robust mit einem IC50 von 11 μM, beeinflusst PKA jedoch nur schwach.

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GKI-1 Chemische Struktur

Cas No.: 2444764-03-6

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5mg
414,00 $
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10mg
689,00 $
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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents Related Products

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].

GKI-1 inhibits full-length human GWL, and shows cellular efficacy[1]. Treatment of HeLa cells (25 and 50 µM) with GKI-1 reduces ENSA/ARPP19 phosphorylation levels, resulting in a decrease in mitotic events, mitotic arrest/cell death and cytokinesis failure[1].

[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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