221243-82-9|1-Naphthyl PP1|CsnPharm

CAS No.: 221243-82-9

1-Naphthyl PP1/1-萘基PP1 Catalog No. CSN13856

Synonyms: 1-NA-PP 1;PP1 Analog

1-Naphthyl PP1 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).

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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].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.1507 mL
- 15.7536 mL
- 31.5072 mL
- 5 mM
- 0.6301 mL
- 3.1507 mL
- 6.3014 mL
- 10 mM
- 0.3151 mL
- 1.5754 mL
- 3.1507 mL

技术信息

CAS号

221243-82-9

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H19N5

运输

蓝冰

分子量

317.39

别名

1-NA-PP 1;PP1 Analog

溶解度

DMSO	22.61 mg/mL (71.2 mM)
Water	insoluble

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