GSK837149A

Names

[ Name ]:
GSK837149A

[Synonym ]:
N,N'-Di[4-(4-Methyl-pyrimidin-2-ylsulfamoyl)phenyl]-urea

Biological Activity

[Description]:

GSK837149A is a selective inhibitor of human Fatty Acid Synthase (FASN) targeting the KR domain. GSK837149A has reversible inhibition effect on FASN and selectivity for type I FASN (Ki=30 nM). GSK837149A is also a competitive inhibitor of NADPH and a non-competitive inhibitor of acetoacetyl-CoA. GSK837149A can be used for the research of obesity and breast cancer[1][2].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Fatty Acid Synthase (FAS)

Research Areas >> Metabolic Disease

[Target]

Ki: 30 nM (type I FASN)[1]

[In Vitro]

GSK837149A (0.1 nM-0.1 mM) 对乙酰辅酶 A/丙二酰辅酶 A 和乙酰乙酰辅酶 A 的抑制作用随作用浓度增加而增强[1]。

[References]

[1]. Vázquez MJ, et al. Discovery of GSK837149A, an inhibitor of human fatty acid synthase targeting the beta-ketoacyl reductase reaction. FEBS J. 2008 Apr;275(7):1556-1567.

[2]. Singha PK, et al. Evaluation of FASN inhibitors by a versatile toolkit reveals differences in pharmacology between human and rodent FASN preparations and in antiproliferative efficacy in vitro vs. in situ in human cancer cells. Eur J Pharm Sci. 2020 Apr 7;149:105321.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₃H₂₂N₈O₅S₂

[ Molecular Weight ]:
554.60100

[ Exact Mass ]:
554.11500

[ PSA ]:
201.79000

[ LogP ]:
5.58260

[ Storage condition ]:
2-8°C

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H319

[ Precautionary Statements ]:
P305 + P351 + P338

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Gloves

[ Hazard Codes ]:
Xi

[ RIDADR ]:
NONH for all modes of transport