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ChemicalBook--->CAS DataBase List--->143984-17-2

143984-17-2

143984-17-2 Structure

143984-17-2 Structure
IdentificationBack Directory
[Name]

Y-29794 tosylate
[CAS]

143984-17-2
[Synonyms]

Y-29794 tosylate
(2-((8-(dimethylamino)octyl)thio)-6-isopropylpyridin-3-yl)(thiophen-2-yl)methanone 4-methylbenzenesulfonate
[Molecular Formula]

C30H42N2O4S3
[MDL Number]

MFCD30533391
[MOL File]

143984-17-2.mol
[Molecular Weight]

590.86
Hazard InformationBack Directory
[Description]

Y-29794 Tosylate is an orally active, potent and specific non-peptide prolyl endopeptidase (PPCE) inhibitor. Y-29794 selectively and competitively inhibited rat brain PPCE (Ki = 0.95 nM) in a reversible manner. Ex vivo study demonstrated that Y-29794 could penetrate into brain to exhibit dose-dependent and long-lasting inhibition. Furthermore, Y-29794 could potentiate the effect of TRH on the release of ACh in the rat hippocampus. Y-29794 prevents the progression of A beta-like deposition in the hippocampus of the SAM.
[Uses]

Y-29794 tosylate is a selective, orally active inhibitor for non-peptide prolyl endopeptidase (PREP), with an IC50 of 3 nM and a Ki 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 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].

Animal Model:TNBC xenograft NOD-SCID mice model[1]
Dosage:12.5-50 mg/kg
Administration:i.p., daily, 5 times a week for 5 weeks
Result:Inhibited tumor growth, maintained body weight.
[IC 50]

PREP: 3 nM (IC50)
[References]

[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. DOI:10.1080/15384047.2020.1824989
[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. DOI:10.1016/0304-3940(92)90884-a
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