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PFM39

Cat. No. M8696
PFM39 Structure
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Biological Activity

PFM39 is a potent cell-permeable Mirin analog that selectively inhibits MRE11 exo-, but not endo-, nuclease activity. PFM39 targets MRE11 in a fashion similar to Mirin, but distinct from that of PFM01 to allow a blockage of dsDNA phosphate backbone rotation and selective inhibition against MRE11 exo-, but not endo-, nuclease activity. FM39 potently impairs G2-phase double-strand break (DSB) repair in 1BR3-hTERT fibrolasts following ionizing irradiation (IR).

Chemical Information
Molecular Weight 219.26
Formula C10H9N3OS
CAS Number 1310744-67-2
Solubility (25°C) DMSO: 15 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] Lea Vlkening, et al. RAD50 regulates mitotic progression independent of DNA repair functions

[2] Atsushi Shibata, et al. DNA double-strand break repair pathway choice is directed by distinct MRE11 nuclease activities

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