GSK837149A_product_DataBase

Bioactivity	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].
Target	Ki: 30 nM (type I FASN)
Invitro	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]。
Name	GSK837149A
CAS	13616-29-0
Formula	C23H22N8O5S2
Molar Mass	554.60
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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.

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