CRT5

Product Name: CRT5
CAS No.: 1034297-58-9
Chemical Name: CRT5
Synonyms: CRT5;CRT5 (CRT0066051);CRT5, protein kinase D inhibitor;3-[6-amino-5-(6-ethoxynaphthalen-2-yl)pyridin-3-yl]-N-[2-(dimethylamino)ethyl]benzamide;Benzamide, 3-[6-amino-5-(6-ethoxy-2-naphthalenyl)-3-pyridinyl]-N-[2-(dimethylamino)ethyl]-
CBNumber: CB53067542
Molecular Formula: C28H30N4O2
Formula Weight: 454.56
MOL File: 1034297-58-9.mol

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CRT5 Property

Boiling point:: 651.2±55.0 °C(Predicted)
Density: 1.173±0.06 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: ≤2.5mg/ml in DMSO;0.25mg/ml in dimethyl formamide
form: crystalline solid
pka: 14.23±0.46(Predicted)

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 18532
Product name: CRT5
Purity: ≥98%
Packaging: 1mg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 18532
Product name: CRT5
Purity: ≥98%
Packaging: 5mg
Price: $139
Updated: 2024/03/01

Cayman Chemical

Product number: 18532
Product name: CRT5
Purity: ≥98%
Packaging: 10mg
Price: $243
Updated: 2024/03/01

Cayman Chemical

Product number: 18532
Product name: CRT5
Purity: ≥98%
Packaging: 25mg
Price: $533
Updated: 2024/03/01

TRC

Product number: C782015
Product name: CRT5
Packaging: 25mg
Price: $415
Updated: 2021/12/16

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CRT5 Chemical Properties,Usage,Production

Description

Protein kinase D (PKD) is a serine/threonine protein kinase that is activated by diacylglycerol, commonly downstream of PKC signaling. The three human PKD isoforms target a variety of proteins to alter cell proliferation, survival, invasion, and protein transport. CRT5 is a pyrazine benzamide that prevents activation of all three isoforms of PKD in endothelial cells treated with VEGF (IC₅₀s = 1, 2, and 1.5 nM for PKD1, PKD2, and PKD3, respectively). It has little effect on a panel of additional kinases when given at 1 μM. CRT5 blocks phosphorylation of PKD1 on Ser⁹¹⁶ and PKD2 on Ser⁸⁷⁶, but does not affect PKC-dependent PKD phosphorylation or PKD autophosphorylation. It also decreases VEGF-induced endothelial migration, proliferation, and tubulogenesis.

Uses

CRT5 is used in the characterization of biological effects of a novel protein kinase D inhibitor in endothelial cells.

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].

References

[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.

CRT5 Preparation Products And Raw materials

Raw materials

Preparation Products

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CRT5 Suppliers

China 39 United Kingdom 1 United States 7 Global 47

Shanghai Lollane Biological Technology Co.,Ltd.

Tel: 021-52996696，15000506266 15000506266
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Pharmacodia (Beijing) Co.,Ltd

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Shanghai EFE Biological Technology Co., Ltd.

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ShangHai Biochempartner Co.,Ltd

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Amadis Chemical Company Limited

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Email: sales@amadischem.com
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Lynnchem

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Email: info@lynnchem.com
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Novachemistry

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TargetMol Chemicals Inc.

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InvivoChem

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Career Henan Chemica Co

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1034297-58-9, CRT5Related Search:

CRT5

Benzamide, 3-[6-amino-5-(6-ethoxy-2-naphthalenyl)-3-pyridinyl]-N-[2-(dimethylamino)ethyl]-

CRT5 (CRT0066051)

3-[6-amino-5-(6-ethoxynaphthalen-2-yl)pyridin-3-yl]-N-[2-(dimethylamino)ethyl]benzamide

CRT5, protein kinase D inhibitor

1034297-58-9