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Merck
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Documentos clave

G5547

Sigma-Aldrich

GSK837149A

≥98% (HPLC), solid

Sinónimos:

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

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About This Item

Fórmula empírica (notación de Hill):
C23H22N8O5S2
Número de CAS:
13616-29-0
Peso molecular:
554.60
Número MDL:
MFCD00133992
Código UNSPSC:
51111800
NACRES:
NA.77

Nivel de calidad

100

Ensayo

≥98% (HPLC)

Formulario

solid

color

white to off-white

solubilidad

DMSO: >10 mg/mL
H2O: insoluble

emisor

GlaxoSmithKline

temp. de almacenamiento

2-8°C

Acciones bioquímicas o fisiológicas

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.

Características y beneficios

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

Pictogramas

Exclamation mark
GHS07

Palabra de señalización

Warning

Frases de peligro

H319

Clasificaciones de peligro

Eye Irrit. 2

Código de clase de almacenamiento

11 - Combustible Solids

Clase de riesgo para el agua (WGK)

WGK 2

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable

Equipo de protección personal

dust mask type N95 (US), Eyeshields, Gloves

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Certificados de análisis (COA)

Lot/Batch Number
125M4616V
098K4620

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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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