GSK180736A MedChemExpress (MCE)

Product Name	GSK180736A
Synonyms	CS-2541 GSK180736 GSK180736A GSK180736A (GSK180736) GRK2 inhibitor GS180736A 5-Pyrimidinecarboxamide, 4-(4-fluorophenyl)-1,2,3,4-tetrahydro-N-1H-indazol-5-yl-6-methyl-2-oxo- 4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
CAS	817194-38-0
EINECS
Chemical Formula	C19H16FN5O2
Molecular Weight	365.36
inchi
Package	10 mM * 1 mL;10 mM * 1 mL;2 mg;2 mg;5 mg;5 mg;10 mg;10 mg;50 mg;50 mg
Price	Email to quote
Descriptions	GSK180736A GSK180736A MedChemExpress (MCE) HY-18990 817194-38-0 98.81% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions GSK180736A GSK180736A MedChemExpress (MCE) HY-18990 817194-38-0 98.81% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. GSK180736A is potent Rho-associated coiled-coil kinase 1 (ROCK1) inhibitor with an IC50 of 100 nM. GSK180736A is also a selective and ATP-competitive G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM. 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 μM 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 μM, but highly potent against ROCK1 (IC50=100 nM)[1]. Cardiac myocytes are isolated from LV free wall and septum of C57/Bl6 mice. Cells are treated with isoproterenol (0.5 μM) for 2 min for the recording of contraction, with pretreatment of either PBS as vehicle or paroxetine (10 μM), 215022 (0.1, 0.5, 1, 10 μM), 215023 (0.1, 0.5, 1, 10 μM), 224064 (0.1, 0.5, 1, 10 μM), and GSK180736A ( 0.5, 1 μM), for 10 min[1]. ROCK1 100 nM (IC50) GRK2 770 nM (IC50) \| \| \| \| \| \| \| \| \| \| [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. [Content Brief]
Last Update	2025-04-01 14:45:47

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