681677

Wnt Pathway Inhibitor XII

The Wnt Pathway Inhibitor XII controls the biological activity of Wnt Pathway. This small molecule/inhibitor is primarily used for Cancer applications.

• Synonym(s): Wnt Pathway Inhibitor XII, (E)-4-(2,6-Difluorostyryl)-N,N-dimethylaniline, FIDAS3, MAT2A Inhibitor I, Methionine S-Adenosyltransferase 2A Inhibitor I
• Empirical Formula (Hill Notation): C₁₆H₁₅F₂N
• CAS Number: 1266684-01-8
• Molecular Weight: 259.29
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: off-white to pale yellow
• solubility: DMSO: 50 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C

Description

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.).

Packaging

Packaged under inert gas

Warning

Toxicity: Regulatory Review (Z)

Other Notes

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

Legal Information

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable