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MilliporeSigma™ Calbiochem™ p38 MAP Kinase Inhibitor XX, FGA-19

Catalog No. 5304860001 Shop All MilliporeSigma Products
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53-048-60001 10 mg
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Catalog No. 53-048-60001 Supplier MilliporeSigma™ Supplier No. 5.30486.0001

Description

A cell-permeable compound that targets p38 C-terminal docking domain. Selectively inhibits MEF-2A phosphorylation by activated p38α (IC50 = 6.31μM)

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 = 6.31μM; [p38] = 1 nM, [MEF-2a] = 10 nM, [ATP] = 25μM) 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 5μM; 1 h drug preincubation), while reduced inhibition against JNK1 and Erk1/2 is only observed at a high concentration of 5μM. 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 (1μg/5μL/mouse), but not SB203580 (up to 5μg/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 .
TRUSTED_SUSTAINABILITY

Specifications

Color Orange Red
Description 98% by HPLC
Target Proteins p38 MAPK
Molecular Formula C13H9ClN4O3
Solubility DMSO
Content And Storage Protect from light
Form Powder
Quantity 10 mg
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