General description

A cell-permeable fluorinated N,N-dialkylaminostilbene (FIDAS) compound that inhibits MAT2A-catalyzed SAM (S-adenosylmethionine) synthesis (IC₅₀ =4.9 µM; [L-Met] = [ATP] = 1 mM, [MAT2A] = 10 µg/mL; 20 min preincubation prior to 30 min reaction) by targeting SAM-binding pocket at the MAT2A dimer interface. Shown to downregulate intracellular SAM level (by 64%; 36 h;10 µM) and Wnt signaling in LS174 CRC (colorectal cancer) cultures and is at least 10-fold more potent than its analogs Pterostilbene (Cat. No. 523310) and Resveratrol (Cat. No. 554325) in inhibiting LS174 proliferation both in vitro (by 70%, 85%, and 90% in 4 d, respectively, with 0.1, 0.3, and 1 µM inhibitor) and in mice in vivo (by 75% on d26; 20 mg/kg/day; i.p.).

A cell-permeable fluorinated N,N-dialkylaminostilbene (FIDAS) compound that inhibits MAT2A-catalyzed SAM (S-adenosylmethionine) synthesis by targeting SAM-binding pocket at the MAT2A dimer interface. Shown to downregulate intracellular SAM level (by 64%; 36 h;10 µM) and Wnt signaling in LS174 colorectal cancer cultures and is at least 10-fold more potent than Pterostilbene (Cat. No. 523310) and Resveratrol (Cat. No. 554325) in inhibiting LS174 proliferation both in vitro (by 90% in 4 d; 1 µM) and in mice in vivo (by 75% on d26; 20 mg/kg/day; i.p.).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Zhang, W., et al. 2013. ACS Chem.Biol.18, In press.Zhang, W., et al. 2011. J. Med. Chem.54, 7579.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Warning

Toxicity: Regulatory Review (Z)