GSK180736A |
Catalog No.GC19177 |
GSK180736A est un puissant inhibiteur de la kinase 1 enroulée associée À Rho (ROCK1) avec une IC50 de 100 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 817194-38-0
Sample solution is provided at 25 µL, 10mM.
GSK180736A is a G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 uM.
GSK180736A is a compound structurally similar to paroxetine that is developed as a ROCK inhibitor, is shown to be an even more potent and selective inhibitor of GRK2 with an IC50 of 0.77 uM and more than 100-fold selectivity over other GRKs. ROCK1 is a potential therapeutic target in the treatment of cardiovascular diseases such as hypertension. GSK180736A is a weak inhibitor of PKA with an IC50 of 30 uM, but highly potent against ROCK1 (IC50=100 nM)[1].
References:
[1]. Waldschmidt HV, et al. Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. J Med Chem. 2016 Apr 28;59(8):3793-807.
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