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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 |
| 2MG | 225 | Get Quote |
|
| 5MG | 353 | Get Quote |
|
| 10MG | 528 | Get Quote |
|
| 25MG | 824 | Get Quote |
|
| 50MG | 1122 | Get Quote |
|
| 100MG | 1485 | Get Quote |
|
| 500MG | Get Quote | Get Quote |
|
| 1G | Get Quote | Get Quote |
|
Biological Information
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Product NameGKI-1
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NoteResearch use only, not for human use.
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Brief DescriptionGKI-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.
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DescriptionGKI-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.
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In VitroGKI-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.
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In Vivo——
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Synonyms——
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PathwayOthers
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TargetOther Targets
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RecptorOthers
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Research Area——
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Indication——
Chemical Information
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CAS Number2444764-03-6
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Formula Weight269.73
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Molecular FormulaC15H12ClN3
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 200 mg/mL (741.48 mM; Ultrasonic )
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SMILESN(C=1C=C(C=CC1)C=2C=NNC2)C3=CC=C(Cl)C=C3
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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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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