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p38 MAPK-IN-4

Chemical Structure : p38 MAPK-IN-4

CAS No.: 1006378-90-0

p38 MAPK-IN-4

Catalog No.: PC-43250Not For Human Use, Lab Use Only.

p38 MAPK-IN-4 is a potent and selective inhibitor of p38 MAPK with IC50 of 68 nM for p38α, inhibits LPS-induced TNFα release in THP-1 cells with IC50 of 187 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

p38 MAPK-IN-4 is a potent and selective inhibitor of p38 MAPK with IC50 of 68 nM for p38α, inhibits LPS-induced TNFα release in THP-1 cells with IC50 of 187 nM; displays no signigicant activity against a panel of 54 tyrosine kinases and serine/threonine kinases; dose-dependently inhibits TNFα production with an ED50 of 0.5 mg/kg in rat-LPS induced TNFα model, dose-dependently inhibits arthritis progression with ED50 <1 mg/kg, demonstrates a superior efficacy of 4 versus other clinically tested reference compounds like BIRB-796 and VX-745.

Physicochemical Properties

M.Wt 349.3534
Formula C21H15F2N2O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1,7-Naphthyridine, 4-(2,4-difluorophenyl)-8-(2-methylphenyl)-, 7-oxide

References

1. Lumeras W, et al. J Med Chem. 2011 Nov 24;54(22):7899-910.

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