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WRN inhibitor 1

Cat. No. M41462
WRN inhibitor 1 Structure
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Biological Activity

WRN inhibitor 1 is a Wemer Syndrome ATP dependent helicase enzyme (WRN) inhibitor that inhibits WRN helicase domain activity.

Chemical Information
Molecular Weight 348.35
Formula C16H13FN2O4S
CAS Number 2923008-44-8
Form Solid
Storage 4°C, protect from light, dry, sealed
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] Joseph A Newman et al. Life Sci Alliance. Structure of the helicase core of Werner helicase, a key target in microsatellite instability cancers

[2] Edmond M Chan et al. Nature. WRN helicase is a synthetic lethal target in microsatellite unstable cancers

[3] Joshua A Sommers et al. PLoS One. A high-throughput screen to identify novel small molecule inhibitors of the Werner Syndrome Helicase-Nuclease (WRN)

[4] Arielle L Heeke et al. JCO Precis Oncol. Prevalence of Homologous Recombination-Related Gene Mutations Across Multiple Cancer Types

[5] Elena Castro et al. BMC Cardiovasc Disord. WRN polymorphisms affect expression levels of plasminogen activator inhibitor type 1 in cultured fibroblasts

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