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      1-Naphthyl PP1 (hydrochloride

      發(fā)布日期:2017-11-02   瀏覽次數:0
      核心提示:a href=https://www.medchemexpress.com/1-Naphthyl-PP1-hydrochloride.html1-Naphthyl PP1 (hydrochloride)/a產品描述:1-Napht
      1-Naphthyl PP1 (hydrochloride)產品描述:1-Naphthyl PP1(1-NA-PP1) hydrochloride 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).IC50 Value:1.0 uM (v-Src); 0.6 uM (c-Fyn); 18 uM (c-Abl) [1]Target: Src Family kinase1-NA-PP1 was considerably more potent and showed distinct substituent effects at the pyrazolopyrimidine core. 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


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      產品鏈接:www.medchemexpress.cn/1-naphthyl-pp1-hydrochloride.html

       
       
       
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