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CRT5

 
Catalog No.
C4165
PKD1、PKD2和PKD3抑制剂
组合的产品项目
规格价格库存 数量
5mg
¥ 2,654.00
Ship with 10-15 days
10mg
¥ 4,170.00
Ship with 10-15 days
25mg
¥ 7,962.00
Ship with 10-15 days

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A

背景

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.

化学属性

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt454.6
Cas No.1034297-58-9
FormulaC28H30N4O2
SynonymsCRT0066051
Solubility≤2.5mg/ml in DMSO;0.25mg/ml in dimethyl formamide
Chemical Name3-[6-amino-5-(6-ethoxy-2-naphthalenyl)-3-pyridinyl]-N-[2-(dimethylamino)ethyl]-benzamide
SDFDownload SDF
Canonical SMILESCCOC1=CC=C2C(C=CC(C3=CC(C4=CC(C(NCCN(C)C)=O)=CC=C4)=CN=C3N)=C2)=C1
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质量控制

质量控制和MSDS

批次:

化学结构

CRT5