KYP-2047 是一种有效的可透过血脑屏障的脯氨酸寡肽酶 (POP) 抑制剂，其 Ki值为 0.023 nM。KYP-2047 通过血管生成和凋亡调节来减少胶质母细胞瘤的增殖。
| 生物活性 | KYP-2047 is a potent and BBB-penetratingprolyl-oligopeptidase (POP)inhibitor, with an Kivalue of 0.023 nM. KYP-2047 reduces glioblastoma proliferation through angiogenesis andapoptosismodulation[1][2]. |
体外研究
(In Vitro) | KYP-2047 (0-100 μM) decreases U-87, U-138 and A-172 cell viability in a concentration-dependent manner[2].
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[2].
Cell Proliferation Assay | Cell Line: | U-87, U-138 and A-172 cell[2] | | 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[2] | | 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. |
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体内研究
(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[1].
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[1].
KYP-2047 (0-5 mg/kg) significantly reduces tumor mass and neutrophil infiltration[2].
KYP-2047 (0-5 mg/kg) significantly reduces vascular endothelial-growth-factor (VEGF), CD34, angiopoietins (Ang) and endothelial-nitric-oxide synthase (eNOS) expression[2].
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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