1-Naphthyl PP1 (hydrochloride)
Names
[ CAS No. ]:
956025-47-1
[ Name ]:
1-Naphthyl PP1 (hydrochloride)
[Synonym ]:
1-Naphthyl PP1 (hydrochloride)
Biological Activity
[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].
[Related Catalog]:
[References]
[Related Small Molecules]
Chemical & Physical Properties
[ Molecular Formula ]:
C19H20ClN5
[ Molecular Weight ]:
353.84900
[ Exact Mass ]:
353.14100
[ PSA ]:
69.62000
[ LogP ]:
5.36690
[ Storage condition ]:
2-8℃