Y-29794 tosylate
Based on 1 Customer Validation
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).
For research use only. We do not sell to patients.
- Purity: 99.86%
- CAS No.: 143984-17-2
- Formula: C30H42N2O4S3
- Molecular Weight:590.86
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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PREP 3 nM (IC50) |
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.
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Cell Line:TNBC, BT20, BT549, MDA453, DU4475, MDA 231, MDA468, SUM159PT
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Concentration:0-10 μM
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Incubation Time:4 days
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Result:Inhibited cell proliferation, induced cell death.
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Cell Line:MDA231, MDA468
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Concentration:0-10 μM
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Incubation Time:48 h
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Result:Arrested cell cycle at G1 phase at 0-5 μM, arrested cell cycle at sub G1 phase at 5-10 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:TNBC xenograft NOD-SCID mice model[1]
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Dosage:12.5-50 mg/kg
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Administration:i.p., daily, 5 times a week for 5 weeks
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Result:Inhibited tumor growth, maintained body weight.
Chemical Information
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CAS No. 143984-17-2
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Appearance Solid
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Molecular Weight 590.86
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Formula C30H42N2O4S3
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Color Off-white to light brown
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SMILES
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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Purity & Documentation
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Data Sheet (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
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. [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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)