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 (K_i=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].

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

GSK837149A (0.1 nM-0.1 mM) shows an increasing inhibition effect on acetyl-CoA/malonyl-CoA, and acetoacetyl-CoA^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

554.60

C₂₃H₂₂N₈O₅S₂

13616-29-0

Solid

White to off-white

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

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [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.  [Content Brief]

  [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.  [Content Brief]