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SPC 839 

Cat. No. M29340
SPC 839  Structure
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Quality Control & Documentation
Biological Activity

SPC 839 (compound 10) is an orally active inhibitor of AP-1 and NF-kB mediated transcriptional activation with IC50 of 0.008 μM.

Chemical Information
Molecular Weight 366.39
Formula C18H14N4O3S
CAS Number 219773-55-4
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Lynn Verstrepen, et al. Biochem Pharmacol. Receptor proximal kinases in NF-κB signaling as potential therapeutic targets in cancer and inflammation

[2] Na Ye, et al. J Med Chem. Small molecule inhibitors targeting activator protein 1 (AP-1)

[3] Chun-Ho Park, et al. Bioorg Med Chem Lett. Discovery of thienopyrimidine-based FLT3 inhibitors from the structural modification of known IKKβ inhibitors

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Keywords: SPC 839  supplier, NF-κB, inhibitors, activators


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