| Identification | Back Directory | [Name]
4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | [CAS]
817194-38-0 | [Synonyms]
CS-2541
GSK180736
GSK180736A
GSK180736A (GSK180736)
GSK180736A >=98% (HPLC)
GRK2 inhibitor GS180736A
4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
5-Pyrimidinecarboxamide, 4-(4-fluorophenyl)-1,2,3,4-tetrahydro-N-1H-indazol-5-yl-6-methyl-2-oxo- | [Molecular Formula]
C19H16FN5O2 | [MDL Number]
MFCD30533616 | [MOL File]
817194-38-0.mol | [Molecular Weight]
365.36 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:57.67(Max Conc. mg/mL);157.83(Max Conc. mM)
Ethanol:3.0(Max Conc. mg/mL);8.21(Max Conc. mM) | [form ]
A crystalline solid | [color ]
Light yellow to khaki |
| Hazard Information | Back Directory | [Uses]
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. | [Biological Activity]
GSK180736A (GSK180736) is a Rho-related, coiled-coil protein kinase inhibitor that binds to GRK2 (G protein-coupled receptor kinase 2) with logIC50 of -6.6. The selectivity for GRK2 is more than 400-fold higher than that for GRK1 and GRK5. | [in vitro]
GSK180736A inhibits GRK2 with IC50 of 770 nM, 300-fold more potent than GRK5. It is a weak PKA inhibitor with IC50=30 μM; it is a potent ROCK1 inhibitor (IC50=100 nM). | [target]
| Target | Value | ROCK
(Cell-free assay) | 100 nM | GRK2
(Cell-free assay) | 6.6(pIC50) | [IC 50]
ROCK1: 100 nM (IC50); GRK2: 770 nM (IC50) | [storage]
Store at -20°C | [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. DOI:10.1021/acs.jmedchem.5b02000 |
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Tags:817194-38-0
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