GKI-1
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].
Product Specifications
CAS Number
[2444764-03-6]
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
ROCK
Type
Reference compound
Related Pathways
Cell Cycle/DNA Damage; Cytoskeleton; Stem Cell/Wnt; TGF-beta/Smad
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/GKI-1.html
Purity
99.96
Solubility
DMSO : 200 mg/mL (ultrasonic)
Smiles
ClC(C=C1)=CC=C1NC2=CC(C3=CNN=C3)=CC=C2
Molecular Formula
C15H12ClN3
Molecular Weight
269.73
Precautions
H302, H315, H319, H335
References & Citations
[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.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, stored under nitrogen)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Available Sizes
Curated Selection
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