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1-Naphthyl PP1

Cat. No. M5303
1-Naphthyl PP1 Structure
Synonym:

1-NA-PP 1

Size Price Availability
25mg USD 397  USD397 4-7 Days
50mg USD 647  USD647 4-7 Days
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Quality Control & Documentation
Biological Activity

1-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.

Chemical Information
Molecular Weight 317.39
Formula C19H19N5
CAS Number 221243-82-9
Solubility (25°C) DMSO ≥ 10 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Tandon M, et al. PLoS One. New pyrazolopyrimidine inhibitors of protein kinase d as potent anticancer agents for prostate cancer cells.

[2] Endo S, et al. Biochem Biophys Res Commun. A single amino-acid change in ERK1/2 makes the enzyme susceptible to PP1 derivatives.

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Keywords: 1-Naphthyl PP1, 1-NA-PP 1 supplier, PKC, inhibitors, activators


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