KYP-2047

SKU: orb1219788

Description

KYP-2047 is a very potent, selective Prolyl oligopeptidase (POP) inhibitor.In cell lines, oxidative stress induced a robust aggregation of α-synuclein,and low concentrations of KYP-2047 significantly reduced the number of cells with α-synuclein inclusions while abolishing the colocalization of α-synuclein and PREP. KYP-2047 significantly reduced the amount of aggregated α-synuclein,and it had beneficial effects on cell viability. In the transgenic mice, a 5-day treatment with the PREP inhibitor reduced the amount of α-synuclein immunoreactivity and soluble α-synuclein protein in the brain.

Key Properties

• CAS Number: 796874-99-2
• MW: 339.44
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₅N₃O₂
• SMILES: O=C(CCCc1ccccc1)N1CCC[C@H]1C(=O)N1CCC[C@H]1C#N
• Target: Prolyl oligopeptidase(pop)
• Solubility: In Vitro: DMSO : 100 mg/mL (294.61 mM)

Bioactivity

• In Vivo:
  KYP-2047 (1 or 5 mg/kg, 30 min before daily testing) dose-dependently improved the escape performance (i. e. latency to find the hidden platform and swimming path length) of the young but not the old rats in the water maze. KYP-2047 (9 or 27 μmol/kg; IP; once, 1 or 3 h before decapitation; two daily doses for 10 days) increases neurotensin concentration in the hypothalamus. KYP-2047 (0-5 mg/kg) significantly reduces tumor mass and neutrophil infiltration. KYP-2047 (0-5 mg/kg) significantly reduces vascular endothelial-growth-factor (VEGF), CD34, angiopoietins (Ang) and endothelial-nitric-oxide synthase (eNOS) expression.
• In Vitro:
  KYP-2047 (0-100 μM) decreases U-87, U-138 and A-172 cell viability in a concentration-dependent manner. KYP-2047 (0-100 μM) increases the pro-apoptotic protein Bax, p53 and caspase-3 expression whereas reduces Bcl-2 expression, and reduced significantly TGF-β expression. Cell Proliferation Assay Cell line: U-87, U-138 and A-172 cell. Concentration: 0.01 μM, 0.1 μM, 0.5 μM, 1 μM, 10 μM, 30 μM, 50 μM and 100 μM Incubation time: 24 h. Result: Decreased U-87, U-138 and A-172 cell viability in a concentration-dependent manner. Western blot analysis. Cell line: U-87 cell. Concentration: 0, 50, 100 μM. Incubation time: 24 h. Result: Increased the pro-apoptotic protein Bax, p53 and cleaved-caspase-3 expression, reduced significantly Bcl2 expression, reduced Ang1 and Ang2 expression, and decreased Ki-67 expression.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Prolyl oligopeptidase(pop)