GSK837149A

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].

Product Specifications

CAS Number

[13616-29-0]

Product Name Alternative

MK0364 (1R,2R)stereoisomer

UNSPSC

12352005

Hazard Statement

H319

Target

Fatty Acid Synthase (FASN)

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/gsk837149a.html

Purity

99.0

Solubility

DMSO : 10 mg/mL (ultrasonic)

Smiles

O=C(NC1=CC=C(C=C1)S(=O)(NC2=NC=CC(C)=N2)=O)NC3=CC=C(C=C3)S(=O)(NC4=NC=CC(C)=N4)=O

Molecular Formula

C23H22N8O5S2

Molecular Weight

554.60

Precautions

H319

References & Citations

[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.