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Chemical Structure : GKI-1
CAS No.: 2444764-03-6
Catalog No.: PC-20557Not For Human Use, Lab Use Only.
GKI-1 (Greatwall Kinase Inhibitor-1) is a specific small-molecule inhibitor of MASTL (microtubule-associated serine/threonine kinase-like, Greatwall/GWL) with IC50 of 10.2 uM.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $248 | In stock | |
| 25 mg | $498 | In stock | |
| 100 mg | $988 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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GKI-1 (Greatwall Kinase Inhibitor-1) is a specific small-molecule inhibitor of MASTL (microtubule-associated serine/threonine kinase-like, Greatwall/GWL) with IC50 of 10.2 uM.
GKI-1 inhibits hGWLFL and hGWL-KinDom with IC50 of 4.9 and 2.5 μM respectively.
GKI-1 displays 2-fold selectivity for binding to hGWLFL over ROCK1, and > 8-fold selectivity over PKA.
GKI-1 reduces ENSA/ARPP19 phosphorylation levels in HeLa cells, resulting in a decrease in mitotic events, mitotic arrest/cell death and cytokinesis failure, which is comparable to siRNA depletion of GWL.
| M.Wt | 269.73 | |
| Formula | C15H12ClN3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
ClC1=CC=C(NC2=CC=CC(C3=CNN=C3)=C2)C=C1 |
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1. Ocasio CA, et al. Oncotarget. 2016 Nov 1;7(44):71182-71197.
2. Kim AY, et al. Front Oncol. 2020 Sep 29;10:571601.
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