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| GSK837149A Basic information |
| Product Name: | GSK837149A | | Synonyms: | GSK837149A;N,N′-Di[4-(4-Methyl-pyrimidin-2-ylsulfamoyl)phenyl]-urea;GSK837149;N,N'-bis-(4-methyl-pyrimidin-2-yl)-4,4'-carbonyldiamino-bis-benzenesulfonamide;4,4'-(Carbonylbis(azanediyl))bis(N-(4-methylpyrimidin-2-yl)benzenesulfonamide);Benzenesulfonamide, 4,4'-(carbonyldiimino)bis[N-(4-methyl-2-pyrimidinyl)-;GSK837149A >=98% (HPLC), solid | | CAS: | 13616-29-0 | | MF: | C23H22N8O5S2 | | MW: | 554.6 | | EINECS: | | Product Categories: | | Mol File: | 13616-29-0.mol |
| GSK837149A Chemical Properties |
| Melting point | 270 °C | | density | 1.568±0.06 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | DMSO: >10mg/mL | | pka | 6.43±0.10(Predicted) | | form | solid | | color | white to off-white |
| Hazard Codes | Xi | | Risk Statements | 36 | | Safety Statements | 26 | | WGK Germany | 2 |
| GSK837149A Usage And Synthesis |
| 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. |
| GSK837149A Preparation Products And Raw materials |
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