530486 Sigma-Aldrichp38 MAP Kinase Inhibitor XX, FGA-19 - Calbiochem

This product has been discontinued.

A cell-permeable, benzoxadiazole compound designed to target p38 c-terminal "docking domain" that mediates interactions with upstream regulators and downstream substrates outside p38 active center. Selectively inhibits MEF-2A phosphorylation by activated p38α (IC₅₀ = 6.31 µM; [p38] = 1 nM, [MEF-2a] = 10 nM, [ATP] = 25 µM) with little or no potency against a panel of other kinases or the docking site interaction-independent MBP phosphorylation by p38. Shown to inhibit LPS-stimulated phosphorylation of p38, MK2, and Hsp27 in THP-1 cells (1 to 5 µM; 1 h drug preincubation), while reduced inhibition against JNK1 & Erk1/2 is only observed at a high concentration of 5 µM. Although SB203580 (Cat. Nos. 559389, 559395, and 559398) exhibits similar potency as FGA-19 in inhibiting LPS-induced TNFα secretion in THP-1 cultures in vitro, only FGA-19 (1 µg/5 µL/mouse), but not SB203580 (up to 5 µg/mouse), intrathecal injection results in lasting (>5 days) reduction of heat sensitivity of paws received carrageenan injection among either wild-type or LysM-GRK2^+/- mice in vivo.