FIDAS-3

Biological Activity

FIDAS-3 is a stilbene derivative and is a potent Wnt inhibitor with an IC50 of 4.9 μM for methionine S-adenosyltransferase 2A (MAT2A). FIDAS-3 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-3 has anticancer activities[1][2]. FIDAS-3 (3 μM; 7 days; LS174T cells) treatment significantly inhibits the proliferation of LS174T cells[1]. FIDAS-3 (3-10 μM) treatment inhibits the expression of c-Myc and cyclinD1 in LS174T CRC cells. And FIDAS-3 induces the expression of cell cycle inhibitor, p21WAF1/CIP1[1]. FIDAS-3 (10 μM; 36 h) treatment reduces the levels of both S-adenosylmethionine (SAM) and S-adenosylhomocysteine (SAH) in LS174T cells[1]. FIDAS-3 (20 mg/kg; intraperitoneal injection; daily; for one months; C57BL/6J athymic nude mice) treatment significantly inhibits the growth of xenograft tumors[2].

References

[1]. Zhang W, et al. Fluorinated N,N-dialkylaminostilbenes repress colon cancer by targeting methionine S-adenosyltransferase 2A. ACS Chem Biol. 2013 Apr 19;8(4):796-803. [2]. Zhang W, et al. Fluorinated N,N-dialkylaminostilbenes for Wnt pathway inhibition and colon cancer repression. J Med Chem. 2011 Mar 10;54(5):1288-97.