FIDAS-5

FIDAS-5 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-5 has anticancer activities. FIDAS-5 is a potent and orally active methionine S-adenosyltransferase 2A (MAT2A) inhibitor with an IC50 of 2.1 μM.FIDAS-5 induces the expression of cell cycle inhibitor, p21WAF1/CIP1. FIDAS-5 (3 μM; 36 h) treatment reduces the levels of both S-adenosylmethionine (SAM) and S-adenosylhomocysteine (SAH) in LS174T cells.FIDAS-5 (3 μM; 7 days; LS174T cells) treatment significantly inhibits the proliferation of LS174T cells. FIDAS-5 (3 μM) treatment inhibits the expression of c-Myc and cyclinD1 in LS174T CRC cells. Mice are treated with FIDAS-5 (20 mg/kg) for 1 week. The liver SAM levels are significantly reduced.FIDAS-5 (20 mg/kg; oral gavage; daily; for two weeks; athymic nude mice) treatment significantly inhibits the growth of xenograft tumors, with minimal difference in body weight.