| CAS NO: | 1034297-58-9 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Cas No. | 1034297-58-9 |
| 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℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 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: |
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