Wnt Pathway Inhibitor XII - Calbiochem

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.).