|
|
| Product Name: | CRT5 | | Synonyms: | CRT5;Benzamide, 3-[6-amino-5-(6-ethoxy-2-naphthalenyl)-3-pyridinyl]-N-[2-(dimethylamino)ethyl]-;CRT5 (CRT0066051) | | CAS: | 1034297-58-9 | | MF: | C28H30N4O2 | | MW: | 454.56 | | EINECS: | | | Product Categories: | | | Mol File: | 1034297-58-9.mol |  |
| 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) |
| 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 |
|