| Identification | Back 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 Information | Back 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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| Company Name: |
BOC Sciences
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| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
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