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Merck
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Key Documents

G5547

Sigma-Aldrich

GSK837149A

≥98% (HPLC), solid

别名:

N,N′-Di[4-(4-Methyl-pyrimidin-2-ylsulfamoyl)phenyl]-urea

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About This Item

经验公式(希尔记法):
C23H22N8O5S2
CAS号:
分子量:
554.60
分類程式碼代碼:
51111800
NACRES:
NA.77

品質等級

化驗

≥98% (HPLC)

形狀

solid

顏色

white to off-white

溶解度

DMSO: >10 mg/mL
H2O: insoluble

起源

GlaxoSmithKline

儲存溫度

2-8°C

生化/生理作用

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.

特點和優勢

This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

象形圖

Exclamation mark

訊號詞

Warning

危險聲明

危險分類

Eye Irrit. 2

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 2

閃點(°F)

Not applicable

閃點(°C)

Not applicable

個人防護裝備

dust mask type N95 (US), Eyeshields, Gloves


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Information on fatty acid synthesis and metabolism in cancer cells. Learn how proliferatively active cells require fatty acids for functions such as membrane generation, protein modification, and bioenergetic requirements. These fatty acids are derived either from dietary sources or are synthesized by the cell.

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