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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
  • Current batch:
  • Purity >98.5%
  • COA
  • MSDS
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 317.39
Formula C19H19N5
CAS Number 221243-82-9
Purity >98.5%
Solubility DMSO ≥ 10 mg/mL
Storage at -20°C
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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  Catalog
Abmole Inhibitor Catalog 2017




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

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