Y-29794 (tosylate)

Y-29794 tosylate is a selective, orally active inhibitor for non-peptide prolyl endopeptidase (PREP), with an IC₅₀ of 3 nM and a K_i of 0.95 nM. Y-29794 tosylate enhances the effect of thyrotropin-releasing hormone (TRH) on the release of ACh in the rat hippocampus, exhibits potential neuroprotective efficacy. Y-29794 tosylate exhibits anticancer activity through inhibition of the IRS1-AKT-mTORC1 pathway. Y-29794 tosylate penetrates the brain-blood barrier (BBB)^[1][2]. In Vitro:Y-29794 tosylate inhibits proliferations of TNBC cancer cells BT20, BT549, MDA453, DU4475, MDA 231, MDA468 and SUM159PT (0-10 μM, 4 days), arrest cell cycle at G1/sub G1 pahse (0-10 μM, 48 h), induces cell death (5-10 mM)^[1].
In Vivo:Y-29794 tosylate (12.5-50 mg/kg, i.p. daily, 5 times a week for 5 weeks) exhibits antitumor efficacy against triple-negative breast cancer in NOD-SCID mice models, without significant toxicity^[1].