4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide Basic information
- Product Name:
- 4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
- Synonyms:
-
- 4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
- GSK180736A
- CS-2541
- GRK2 inhibitor GS180736A
- GSK180736
- GSK180736A (GSK180736)
- 5-Pyrimidinecarboxamide, 4-(4-fluorophenyl)-1,2,3,4-tetrahydro-N-1H-indazol-5-yl-6-methyl-2-oxo-
- GSK180736A >=98% (HPLC)
- CAS:
- 817194-38-0
- MF:
- C19H16FN5O2
- MW:
- 365.36
- Product Categories:
-
- API
- Mol File:
- 817194-38-0.mol
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4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide Chemical Properties
- 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
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4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide Usage And Synthesis
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) |