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CRT5 Sale

(Synonyms: CRT0066051) 目录号 : GC14355

A pan PKD inhibitor

CRT5 Chemical Structure

Cas No.:1034297-58-9

规格 价格 库存 购买数量
1mg
¥444.00
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5mg
¥1,951.00
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10mg
¥3,426.00
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25mg
¥7,519.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

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.

Chemical Properties

Cas No. 1034297-58-9 SDF
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°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.1997 mL 10.9987 mL 21.9974 mL
5 mM 0.4399 mL 2.1997 mL 4.3995 mL
10 mM 0.22 mL 1.0999 mL 2.1997 mL
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