CRT5
- Product Name
- CRT5
- CAS No.
- 1034297-58-9
- Chemical Name
- CRT5
- Synonyms
- CRT5;CRT5 (CRT0066051);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
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)
N-Bromosuccinimide Price
- Product number
- 18532
- Product name
- CRT5
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 18532
- Product name
- CRT5
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $139
- Updated
- 2024/03/01
- Product number
- 18532
- Product name
- CRT5
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $243
- Updated
- 2024/03/01
- Product number
- 18532
- Product name
- CRT5
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $533
- Updated
- 2024/03/01
- Product number
- C782015
- Product name
- CRT5
- Packaging
- 25mg
- Price
- $415
- Updated
- 2021/12/16
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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