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Merck

G5547

Sigma-Aldrich

GSK837149A

≥98% (HPLC), solid

Synonym(e):

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

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About This Item

Empirische Formel (Hill-System):
C23H22N8O5S2
CAS-Nummer:
Molekulargewicht:
554.60
MDL-Nummer:
UNSPSC-Code:
51111800
NACRES:
NA.77

Qualitätsniveau

Assay

≥98% (HPLC)

Form

solid

Farbe

white to off-white

Löslichkeit

DMSO: >10 mg/mL
H2O: insoluble

Ersteller

GlaxoSmithKline

Lagertemp.

2-8°C

Biochem./physiol. Wirkung

GSK837149A is a selective inhibitor of human fatty acid synthase (FAS).
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.

Leistungsmerkmale und Vorteile

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

Piktogramme

Exclamation mark

Signalwort

Warning

H-Sätze

Gefahreneinstufungen

Eye Irrit. 2

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 2

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

Persönliche Schutzausrüstung

dust mask type N95 (US), Eyeshields, Gloves


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Prosanta K Singha et al.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 149, 105321-105321 (2020-04-11)
De novo synthesis of fatty acids is essential to maintain intensive proliferation of cancer cells. Unlike normal cells that utilize food-derived circulating lipids for their fuel, cancer cells rely on heightened lipogenesis irrespective of exogenous lipid availability. Overexpression and activity
David Weigt et al.
Cell chemical biology, 26(9), 1322-1331 (2019-07-08)
Human cancers require fatty acid synthase (FASN)-dependent de novo long-chain fatty acid synthesis for proliferation. FASN is therefore an attractive drug target, but fast technologies for reliable label-free cellular compound profiling are lacking. Recently, MALDI-mass spectrometry (MALDI-MS) has emerged as

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