All Photos(1)
Synonym(s):
InSolution p38 MAP Kinase Inhibitor III
Empirical Formula (Hill Notation):
C23H21FN4S
Molecular Weight:
404.50
UNSPSC Code:
12352200
NACRES:
NA.77
Recommended Products
Quality Level
Assay
≥98% (HPLC)
form
liquid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
desiccated (hygroscopic)
protect from light
shipped in
wet ice
storage temp.
2-8°C
General description
A cell-permeable, potent, selective, 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 p38α; 0.16 and 0.039 µM in suppressing LPS-induced TNF-α and IL-1β release, respectively, in human PBMC; ED50 = 1.33 mg/kg in suppressing LPS-induced TNF-α release in mouse
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Physical form
A 10 mM (1 mg/247 µl) solution of p38 MAP Kinase Inhibitor III (Cat. No. 506121) in DMSO.
Reconstitution
Following initial use, aliquot and refrigerate (4°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)
closed cup
Flash Point(C)
closed cup
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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