A cell-permeable furanylcarboxamide compound that acts as a potent, reversible and non-ATP-competitive inhibitor of MK-2/MAPKAP-K2 activity (IC50=110nM; EC50=350nM for pHSP27 in IL-1b-stimulated SW1353 cells) with excellent selectivity over 150 kinases (% activity inhibition at 10uM against human CK2, Haspin, Arg and CK1y3=40, 40, 42 and >70, respectively). Shown to efficiently suppress the secretions of TNFa, IL6 (IC50=4.4 and 5.2uM in LPS-stimulated THP1 cell, respectively) and MMP-13 (IC50=5.7 and 2.2uM in IL1b-stimulated SW1353 and in primary osteoarthritis-derived chondrocytes, respectively). Exhibits desirable bioavailability and weakly inhibits a panel of cytochrome P450 isozymes (IC50>20uM for 3A4, 2D6 and 2C9).
Formula:C27H25ClN4O2, HCl
Solubility:DMSO
Molecular Weight:509.4
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
