Doramapimod ≥99% (durch HPLC), Calbiochem®
Lieferant: Merck Millipore Calbiochem
Synonyme:
p38 MAP Kinase Inhibitor X, 1-(3-(tert-Butyl)-1-(p-tolyl)-1H-pyrazol-5-yl)-3-(4-(2-morpholinoethoxy)naphthalen-1-yl)urea, BIRB 796
p38 MAP kinase inhibitor X, BIRB 796, is a cell-permeable, highly potent, slow binding, high affinity inhibitor of p38a (IC50 = 8 and 97 nM with or without 2 h preincubation).
A cell-permeable pyrazolo-napthalenyl urea compound that acts as a highly potent, slowly binding (IC50 = 8 and 97 nM, respectively, against human p38α, respectively, with or without 2 h preincubation), but high affinity (t1/2 of dissociation from human p38α = 23 h), p38-selective inhibitor by simultaneously targeting the ATP-binding site and an adjacent DFG-out conformation-specific allosteric cavity. It inhibits JNK2α2 and c-Raf-1 only at much higher concentrations (IC50 = 98 nM and 1.4 µM, respectively) and displays little or no activity toward 10 other kinases (IC50 >20 µM). Shown to inhibit LPS-induced TNF-α production both in vitro (IC50 = 18 and 780 nM using THP-1 cells and in human whole blood, respectively) and in mice in vivo (by 84%; 30 mg/kg p.o.).
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Formel:
C₃₁H₃₇N₅O₃ Molecular Weight: 527,669 g/mol Lagertemperatur: Kühlschrank |
MDL:
MFCD09752957 CAS-Nummer: 285983-48-4 |
Spezifikation Testergebnisse
| Purity | ≥99% by HPLC |
| Form | White Solid |
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