"目录号: HY-13941B
1-Naphthyl PP1(1-NA-PP1) 盐酸盐是src家族抑制剂，对v-Src，c-Fyn，c-Abl，CDK2和CAMK II的IC50分别为1.0，0.6，0.6，18和22 μM。
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Dasatinib-Ponatinib-Saracatinib-PP2-Bosutinib-A 419259 trihydrochloride-1-Naphthyl PP1-PP1-DCC-2036-SU6656-WH-4-023-Scutellarein-Src Inhibitor 1-KX2-391 dihydrochloride-XL228-
生物活性
Description
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-sensitive PKD1(M659G) for dissecting PKD-specific functions and signaling pathways in various biological systems [2].
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