1-Naphthyl PP1
产品说明书
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同义名 : | 1-NA-PP 1; PP1 Analog |
| CAS号 : | 221243-82-9 | |
| 货号 : | A252944 | |
| 分子式 : | C19H19N5 | |
| 纯度 : | 99%+ | |
| 分子量 : | 317.39 | |
| MDL号 : | MFCD03425471 | |
| 存储条件： |
Pure form Keep in dark place, inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 12 mg/mL(37.81 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Src and Src-family protein-tyrosine kinases are regulatory proteins that play key roles in cell differentiation, motility, proliferation, and survival[3]. 1-Naphthyl PP1 (1-NA-PP 1) is a selective inhibitor of src family kinases v-Src and c-Fyn as well as the tyrosine kinase c-Abl (IC50 values are 1.0, 0.6, 0.6, 18 and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II respectively)[4]. 1-NA-PP1 was cell-active, and potently blocked prostate cancer cell proliferation by inducing G2/M arrest. Overexpression of PKD1 or PKD3 almost completely reversed the growth arrest and the inhibition of tumor cell invasion caused by 1-NA-PP1, indicating that its anti-proliferative and anti-invasive activities were mediated through the inhibition of PKD. Interestingly, a 12-fold increase in sensitivity to 1-NA-PP1 could be achieved by engineering a gatekeeper mutation in the active site of PKD1, suggesting that 1-NA-PP1 could be paired with the analog-sensitive PKD1(M659G) for dissecting PKD-specific functions and signaling pathways in various biological systems[5]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.15mL 0.63mL 0.32mL |
15.75mL 3.15mL 1.58mL |
31.51mL 6.30mL 3.15mL |
| 参考文献 |
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