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Chemical Structure : AS1940477
Catalog No.: PC-61001Not For Human Use, Lab Use Only.
A potent, selective, orally active p38α/p38β inhibitor with IC50 of 11.2/36.5 nM respectively, with no effect on p38γ and δ isoforms (IC50>1 uM).
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A potent, selective, orally active p38α/p38β inhibitor with IC50 of 11.2/36.5 nM respectively, with no effect on p38γ and δ isoforms (IC50>1 uM); displays no activity against a panel of 100 protein kinases, including JNK2, EGFR, Akt and Pim; inhibits LPS- or PHA-induced production of proinflammatory cytokines, including TNFα, IL-1β, and IL-6 at low concentrations (LPS/TNFα, IC50=0.45 nM; PHA/TNFα, IC50=0.40 nM) in human PBMCs, also inhibits TNFα- and IL-1 β-induced production of IL-6, PGE(2), and MMP-3 in human synovial stromal cells; potently inhibits TNF production in whole blood (IC50=12 nM) and effectively inhibits TNFα production induced by LPS in rats with long-acting anti-inflammatory effect.
| M.Wt | 431.471 | |
| Formula | C24H22FN5O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Asano T, et al. J Med Chem. 2012 Sep 13;55(17):7772-85.
2. Terajima M, et al. Eur J Pharmacol. 2013 Jan 5;698(1-3):455-62.
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