506121
p38 MAP Kinase Inhibitor III
The p38 MAP Kinase Inhibitor III, also referenced under CAS 581098-48-8, controls the biological activity of p38 MAP Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
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Synonym(s):
p38 MAP Kinase Inhibitor III, ML3403, (RS)-{4-[5-(4-Fluorophenyl)-2-methylsulfanyl-3H-imidazol-4-yl]pyridin-2-yl}-(1-phenylethyl)amine]
Empirical Formula (Hill Notation):
C23H21FN4S
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Quality Level
Assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
yellow
solubility
DMSO: 5 mg/mL
shipped in
ambient
storage temp.
2-8°C
InChI
1S/C23H21FN4S/c1-15(16-6-4-3-5-7-16)26-20-14-18(12-13-25-20)22-21(27-23(28-22)29-2)17-8-10-19(24)11-9-17/h3-15H,1-2H3,(H,25,26)(H,27,28)
InChI key
VXPWQNBKEIVYIS-UHFFFAOYSA-N
General description
A cell-permeable methylsulfanylimidazole compound that acts as a potent, selective, reversible, and ATP-competitive p38 MAP kinase inhibitor (IC50 = 0.38 µM for p38α). Shown to effectively suppresses LPS-induced cytokine release both in vitro (IC50 = 0.16 and 0.039 µM for TNF-α and IL-1β release, respectively, in human PBMC) and in vivo (ED50 = 1.33 mg/kg for TNF-α release in mouse). When compared with SB 203580 (Cat. No. 559389 and 559398), it exhibits reduced inhibitory activity against cytochrome P450-2D6 isoform and, therefore, is better suited for in vivo use. A 10 mM (1 mg/247 µl) solution of p38 MAP Kinase Inhibitor III (Cat. No. 506148) in DMSO is also available.
A cell-permeable, potent, selective, reversible, and ATP-competitive inhibitor of p38 MAP kinase (IC50 = 380 nM for p38α). Shown to effectively suppress LPS-induced cytokine release in vitro (IC50 = 160 nM for TNF-α release and 39 nM for IL-1β release, human PBMC) and in vivo (ED50 = 1.33 mg/kg for TNF-α release in mice). Exhibits reduced inhibitory activity against cytochrome P450-2D6 compared to SB 203580 (Cat. No 559389) and is better suited for use in animal models.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
p38 MAP kinase
p38 MAP kinase
Product competes with ATP.
Reversible: yes
Target IC50: 0.38 µM for p38 MAP kinase α; 0.16 and 0.039 µM in suppressing LPS-induced TNF-α and IL-1β release, respectively, in human PBMC
Packaging
Packaged under inert gas
Warning
Toxicity: Carcinogenic / Teratogenic (D)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Laufer, S.A., et al. 2003. J. Med. Chem.46, 3230.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 1
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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