1-Naphthyl PP1

Modify Date: 2024-01-09 09:58:24

1-Naphthyl PP1 Structure
1-Naphthyl PP1 structure
Common Name 1-Naphthyl PP1
CAS Number 221243-82-9 Molecular Weight 317.388
Density 1.3±0.1 g/cm3 Boiling Point 527.8±45.0 °C at 760 mmHg
Molecular Formula C19H19N5 Melting Point 219-222ºC
MSDS N/A Flash Point 273.0±28.7 °C

 Use of 1-Naphthyl PP1


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).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].

 Names

Name 1-na-pp1
Synonym More Synonyms

 1-Naphthyl PP1 Biological Activity

Description 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).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

[1]. Bishop AC, et al. A chemical switch for inhibitor-sensitive alleles of any protein kinase. Nature. 2000 Sep 21;407(6802):395-401.

[2]. Tandon M, et al. New pyrazolopyrimidine inhibitors of protein kinase d as potent anticancer agents for prostate cancer cells. PLoS One. 2013 Sep 23;8(9):e75601.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 527.8±45.0 °C at 760 mmHg
Melting Point 219-222ºC
Molecular Formula C19H19N5
Molecular Weight 317.388
Flash Point 273.0±28.7 °C
Exact Mass 317.164032
PSA 69.62000
LogP 3.88
Vapour Pressure 0.0±1.4 mmHg at 25°C
Index of Refraction 1.688
Storage condition 2-8℃

 Synonyms

1-(2-Methyl-2-propanyl)-3-(1-naphthyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
1-tert-butyl-3-naphthalen-1-ylpyrazolo[3,4-d]pyrimidin-4-amine
4-Amino-1-tert-butyl-3-(1,-naphthyl)pyrazolo[3,4-d]pyrimidine
1-NA-PP1
1H-Pyrazolo[3,4-d]pyrimidin-4-amine, 1-(1,1-dimethylethyl)-3-(1-naphthalenyl)-
1-tert-butyl-3-(1-naphthyl)-1h-pyrazolo[3,4-d]pyrimidin-4-amine
1-Naphthyl PP1
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