KYP-2047

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

KYP-2047 是一种非常有效的选择性脯氨酰寡肽酶 (POP) 抑制剂。在细胞系中，氧化应激诱导 α-突触核蛋白的强烈聚集，低浓度的 KYP-2047 显着减少了具有 α-突触核蛋白包涵体的细胞数量，而废除 α-突触核蛋白和 PREP 的共定位。

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.

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.

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.

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Others

Other Targets

Prolyl oligopeptidase(pop)

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796874-99-2

339.44

C20H25N3O2

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (294.61 mM)

O=C(CCCc1ccccc1)N1CCC[C@H]1C(=O)N1CCC[C@H]1C#N

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(-20℃)

With Ice Pack

≥ 2 years