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CRT5
本半岛bd体育手机客户端 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。
CRT5图片
CAS NO: 1034297-58-9
包装与价格:
包装 价格(元)
1mg 电议
5mg 电议
10mg 电议
25mg 电议

半岛bd体育手机客户端 介绍
CRT5 是一种吡嗪苯甲酰胺,是一种有效的选择性抑制剂,作用于用 VEGF 处理的内皮细胞中的所有三种 PKD 同工型(对 PKD1、PKD2 和 PKD3 的 IC50 分别为 1、2 和 1.5 nM)。
Cas No. 1034297-58-9
别名 CRT0066051
化学名 3-[6-amino-5-(6-ethoxy-2-naphthalenyl)-3-pyridinyl]-N-[2-(dimethylamino)ethyl]-benzamide
Canonical SMILES CCOC1=CC=C2C(C=CC(C3=CC(C4=CC(C(NCCN(C)C)=O)=CC=C4)=CN=C3N)=C2)=C1
分子式 C28H30N4O2
分子量 454.6
溶解度 ≤2.5mg/ml in DMSO;0.25mg/ml in dimethyl formamide
储存条件 Store at -20℃
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
半岛bd体育手机客户端 描述

CRT5 is a novel and specific PKD inhibitor [1]. PKDs (Protein kinase Ds) are DAG (diacylglycerol)-stimulated serine/threonine protein kinases [1]. Three known PKD isoforms have been identified: PKD1–PKD3. PKD acted as an mediator implicated in diverse cellular functions, including proliferation, cellular trafficking, survival and regulation of transcription [1].

In vitro: The non-linear regression analysis revealed that LD50 value of CRT5 was 17 μM. The biochemical IC50 value of CRT5 for PKD1, PKD2 and PKD3 were 1, 2 and 1.5 nM, respectively [1]. CRT5 (1 μM) completely inhibited PKD1 and PKD2, but showed little inhibitory effect on the PKC isoforms. CRT5 significantly reduced VEGF-induced phosphorylation of HSP27 at the position Ser82. CRT5 significantly reduced the migratory response towards VEGF by 42–51%. CRT5 decreased the proliferation of control cells not treated with VEGF to a less extent. VEGF increased HUVEC tubule formation in a collagen-based assay. CRT5 markedly inhibited VEGF-induced tubulogenesis [1].

Reference:
[1] Evans I M, Bagherzadeh A, Charles M, et al. Characterization of the biological effects of a novel protein kinase D inhibitor in endothelial cells[J]. Biochemical Journal, 2010, 429(3): 565-572.

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