13616-29-0
Chemical Structure
GSK837149A
- CAS No.: 13616-29-0
- Formula:C23H22N8O5S2
- Molecular Weight:554.60
IUPAC Name: 4,4'-(carbonylbis(azanediyl))bis(N-(4-methylpyrimidin-2-yl)benzenesulfonamide)
InChIKey: RSINKZJTTORDAJ-UHFFFAOYSA-N
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
Biological Activity: 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].
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GSK837149A | 99.13% | 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. | ||||||||||||||||||||
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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. [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]
