1. Metabolic Enzyme/Protease
  2. Prolyl Endopeptidase (PREP)
  3. 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 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.

Y-29794 tosylate Chemical Structure

Y-29794 tosylate Chemical Structure

CAS No. : 143984-17-2

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Description

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].

IC50 & Target

PREP

3 nM (IC50)

In Vitro

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.

Cell Proliferation Assay[1]

Cell Line: TNBC, BT20, BT549, MDA453, DU4475, MDA 231, MDA468, SUM159PT
Concentration: 0-10 μM
Incubation Time: 4 days
Result: Inhibited cell proliferation, induced cell death.

Cell Cycle Analysis[1]

Cell Line: MDA231, MDA468
Concentration: 0-10 μM
Incubation Time: 48 h
Result: Arrested cell cycle at G1 phase at 0-5 μM, arrested cell cycle at sub G1 phase at 5-10 μM.
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].

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

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.
Molecular Weight

590.86

Formula

C30H42N2O4S3

CAS No.
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Y-29794 tosylate
Cat. No.:
HY-15113A
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