| Identification | Back Directory | [Name]
GSK837149A | [CAS]
13616-29-0 | [Synonyms]
GSK837149
GSK837149A
GSK837149A >=98% (HPLC), solid
N,N′-Di[4-(4-Methyl-pyrimidin-2-ylsulfamoyl)phenyl]-urea
Benzenesulfonamide, 4,4'-(carbonyldiimino)bis[N-(4-methyl-2-pyrimidinyl)-
N,N'-bis-(4-methyl-pyrimidin-2-yl)-4,4'-carbonyldiamino-bis-benzenesulfonamide
4,4'-(Carbonylbis(azanediyl))bis(N-(4-methylpyrimidin-2-yl)benzenesulfonamide) | [Molecular Formula]
C23H22N8O5S2 | [MDL Number]
MFCD11114386 | [MOL File]
13616-29-0.mol | [Molecular Weight]
554.6 |
| Chemical Properties | Back Directory | [Melting point ]
270 °C | [density ]
1.568±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: >10mg/mL | [form ]
solid | [pka]
6.43±0.10(Predicted) | [color ]
white to off-white |
| Hazard Information | Back Directory | [Description]
A number of tumor cells and cell lines have been observed to have highly upregulated expression and activity of fatty acid synthase (FASN). GSK837149A is a selective, reversible inhibitor of FASN (pIC50 = 7.8). It acts by inhibiting the β-ketoacyl reductase activity of FASN. | [Biochem/physiol Actions]
GSK837149A is the first selective inhibitor of human fatty acid synthase (FAS) known to act specifically and selectively on the KR activity of the enzyme. It was first isolated as a minor impurity in a sample found to be active against the enzyme in a high-throughput screening campaign. This compound and its analogs synthesized, all being symmetrical structures containing a bisulfonamide urea, act by inhibiting the beta-ketoacyl reductase activity of the enzyme. GSK837149A inhibits FAS in a reversible mode, with a Ki value of approximately 30 nm, and it possibly binds to the enzyme-ketoacyl-ACP complex. Although initial results suggest that cell penetration for these compounds is impaired, they still can be regarded as useful tools with which to probe and explore the beta-ketoacyl reductase active site in FAS, helping in the design of new inhibitors. |
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Energy Chemical
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