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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

590.86

C₃₀H₄₂N₂O₄S₃

143984-17-2

O=C(C1=CC=C(C(C)C)N=C1SCCCCCCCCN(C)C)C2=CC=CS2.O=S(C3=CC=C(C)C=C3)(O)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Perez RE, et al. Prolyl endopeptidase inhibitor Y-29794 blocks the IRS1-AKT-mTORC1 pathway and inhibits survival and in vivo tumor growth of triple-negative breast cancer. Cancer Biol Ther. 2020 Nov 1;21(11):1033-1040.  [Content Brief]

  [2]. Nakajima T, et al. Y-29794--a non-peptide prolyl endopeptidase inhibitor that can penetrate into the brain. Neurosci Lett. 1992 Jul 20;141(2):156-60.  [Content Brief]