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].
1-Naphthyl PP1/1-萘基PP1 细胞实验
Cell Line
Concentration
Treated Time
Description
References
TFK-1 cells
25.45 μM(IC50)
48 h
Inhibited proliferation of TFK-1 cells
Cells. 2022 Sep 30;11(19):3088
HuCCT1 cells
56.23 μM(IC50)
48 h
Inhibited proliferation of HuCCT1 cells
Cells. 2022 Sep 30;11(19):3088
U2OS cells
10 µM
24 h
To validate the specific inhibitory effect of 1-Na-PP1 on as-AurA, results showed that 10 µM 1-Na-PP1 completely inhibited as-AurA activity but had no effect on wt-AurA.
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