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ARTD3/PARP3-IN-1

Cat. No. M42940
ARTD3/PARP3-IN-1 Structure
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Biological Activity

ARTD3/PARP3-IN-1 is an unselective inhibitor of diphtheria toxin-like ADP-ribosyltransferase 3 (ARTD3)/PARP3.

Chemical Information
Molecular Weight 308.33
Formula C17H16N4O2
CAS Number 730949-09-4
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] Carole Beck et al. Nucleic Acids Res. PARP3 affects the relative contribution of homologous recombination and nonhomologous end-joining pathways

[2] Anders E G Lindgren et al. J Med Chem. Chemical probes to study ADP-ribosylation: synthesis and biochemical evaluation of inhibitors of the human ADP-ribosyltransferase ARTD3/PARP3

[3] Anders E G Lindgren et al. ACS Chem Biol. PARP inhibitor with selectivity toward ADP-ribosyltransferase ARTD3/PARP3

[4] Karla Lh Feijs et al. Cell Commun Signal. ARTD10 substrate identification on protein microarrays: regulation of GSK3β by mono-ADP-ribosylation

[5] Christian Boehler et al. Proc Natl Acad Sci U S A. Poly(ADP-ribose) polymerase 3 (PARP3), a newcomer in cellular response to DNA damage and mitotic progression

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Keywords: ARTD3/PARP3-IN-1 supplier, inhibitors, activators

 
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