An inhibitor of fatty acid synthase (IC50 = 7.7 nM in an assay detecting released CoA); selective for the KR domain over the KS domain of FASN (IC50s = 29 and >10

GSK2194069 – 5 mg

Brand:
Cayman
CAS:
1332331-08-4
Storage:
-20
UN-No:
Non-Hazardous - /

GSK2194069 is an inhibitor of fatty acid synthase (FASN) with an IC50 value of 7.7 nM in an assay detecting released CoA.{35126} It is a competitive inhibitor that is selective for the KR domain over the KS domain of FASN, with IC50 values of 29 and >10,000 nM, respectively, in vitro. GSK2194069 decreases incorporation of 13C-labeled acetate into cellular lipids in a dose-dependent manner in KATO-III, MKN-45, and SNU-1 gastric, and A549 non-small cell lung cancer cell lines. It also reduces cell growth of A549 cells (EC50 = 15 nM) and inhibits lipid synthesis without decreasing FASN protein expression.  

 

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SKU: 20022 - Category:

Description

An inhibitor of fatty acid synthase (IC50 = 7.7 nM in an assay detecting released CoA); selective for the KR domain over the KS domain of FASN (IC50s = 29 and >10,000 nM, respectively); decreases incorporation of 13C-labeled acetate into cellular lipids in a dose-dependent manner in KATO-III, MKN-45, and SNU-1 gastric, and A549 non-small cell lung cancer cell lines; reduces cell growth of A549 cells (EC50 = 15 nM)

Formal name: 4-[4-(5-benzofuranyl)phenyl]-5-[[(3S)-1-(cyclopropylcarbonyl)-3-pyrrolidinyl]methyl]-2,4-dihydro-3H-1,2,4-triazol-3-one

Synonyms: 

Molecular weight: 428.5

CAS: 1332331-08-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer

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