Rofecoxib is a non-steroidal anti-inflammatory drug (NSAID) that selectively inhibits COX-2 over COX-1 with IC50 values of 0.018 and >15 µM, respectively, for production of prostaglandin E2 (PGE2, Cay-14010) in CHO cells expressing the recombinant human enzymes. In vivo, rofecoxib inhibits carrageenan-induced paw...

The transcription factor NF-kappaB plays a key role in regulating over 150 target genes including the expression of inflammatory cytokines, chemokines, immunoreceptors, and cell adhesion molecules. In the cytoplasm, inactive NF-kappaB complexes are bound to an inhibitor IkappaB. However in response to certain...

SC-514 is a selective and reversible inhibitor of IkappaB kinase 2 (IKK2) (IC50 = 3-12 µM) that displays greater than 10-fold selectivity over 28 other kinases, including JNK, p38, MK2, and ERK. In synovial fibroblasts stimulated with interleukin (IL)-1beta, SC-514 attenuates NF-kappaB-mediated expression of IL-6,...

LFM-A13 is an inhibitor of Bruton's tyrosine kinase (BTK, IC50 = 2.5 µM). It is selective for BTK over JAK1, JAK3, IRK, EGFR, and HCK (IC50s = >278 µM for all), as well as a panel of seven serine/threonine and 10 tyrosine kinases as well as one lipid kinase (IC50s = >200-500 µM), but does inhibit polo-like kinase 3...

Lavendustin A is a selective inhibitor of epidermal growth factor (EGF) receptor-associated tyrosine kinase (IC50 = 11 nM) that was first isolated from a Streptomyces culture filtrate. It does not inhibit protein kinase A (PKA), PKC, or PI3K (IC50s > 100 µM). It has been used to differentiate rat mesenchymal stem...