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KYP-2047
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
KYP-2047图片
CAS NO:796874-99-2
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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.
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].

分子量

339.43

Formula

C20H25N3O2

CAS 号

796874-99-2

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.