FIDAS-3

FIDAS-3 is an inhibitor of S-adenosylmethionine synthase isoform type-2 (AdoMet synthase 2; IC₅₀ = 4.9 µM).¹ It also is an inhibitor of human-ether-a-go-go (hERG; IC₅₀ = 32.1 µM in a voltage-clamp assay using HEK293 cells expressing hERG).² FIDAS-3 reduces the proliferation of LS 174T colorectal cancer cells (IC₅₀ = 26.9 µM) and the levels of Axin2 and c-Myc in the same cells when used at a concentration of 10 µM.^1,3 Intraperitoneal administration of FIDAS-3 (20 mg/kg per day) decreases tumor growth in an LS 174T mouse xenograft model.³

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1. Sviripa, V.M., Zhang, W., Balia, A.G., et al. 2',6'-Dihalostyrylanilines, pyridines, and pyrimidines for the inhibition of the catalytic subunit of methionine S-adenosyltransferase-2. J. Med. Chem. 57(14), 6083-6091 (2014).

2. Zhang, W., Sviripa, V., Chen, X., et al. Fluorinated N,N-dialkylaminostilbenes repress colon cancer by targeting methionine S-adenosyltransferase 2A. ACS Chem. Biol. 8(4), 796-803 (2013).

3. Zhang, W., Sviripa, V., Kril, L.M., et al. Fluorinated N,N-dialkylaminostilbenes for Wnt pathway inhibition and colon cancer repression. J. Med. Chem. 54(5), 1288-1297 (2011).