Key Specifications Table
Pricing & Availability
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|5.30486.0001||Glass bottle||10 mg||
|Overview||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.|
|Synonyms||N-(5-Chloro-2-methylphenyl)-7-nitrobenzo[c][1,2,5]oxadiazol-4-amine, FGA 19|
|References||Willemen, H. L., et al. 2014. Biochem. J. 459, 427.|
|Form||Orange red powder|
|Primary Target||p38 MAPK|
|Primary Target IC<sub>50</sub>||6.31 µM for p38 MAPK-mediated phosphorylation of MEF-2A-Thr312|
|Purity||≥98% by HPLC|
|Safety Information according to GHS|
|Product Usage Statements|
|Packaged under inert gas||Packaged under inert gas|
|Willemen, H. L., et al. 2014. Biochem. J. 459, 427.|
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.