Y-29794
Y-29794 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 enhances the effect of thyrotropin-releasing hormone (TRH) on the release of ACh in the rat hippocampus, exhibits potential neuroprotective efficacy. Y-29794 exhibits anticancer activity through inhibition of the IRS1-AKT-mTORC1 pathway. Y-29794 penetrates the brain-blood barrier (BBB).
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- CAS No.: 129184-48-1
- Formule: C23H34N2OS2
- Masse moléculaire:418.66
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
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PREP 3 nM (IC50) |
In Vitro
Y-29794 inhibits proliferations of TNBC cancer cells BT20, BT549, MDA453, DU4475, MDA 231, MDA468 and SUM159PT (0-10 μM, 4 days), arrests 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.
In Vivo
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. 129184-48-1
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Masse moléculaire 418.66
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Formule C23H34N2OS2
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SMILES
O=C(C1=C(SCCCCCCCCN(C)C)N=C(C(C)C)C=C1)C2=CC=CS2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. 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]
[2]. 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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Y-29794 Related Classifications
HY-15113 Related Classifications
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