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559388

Millipore

SB 202190

≥98% (HPLC), solid, p38 MAP kinase inhibitor, Calbiochem®

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Synonym(s):
SB 202190, 4-(4-Fluorophenyl)-2-(4-hydroxyphenyl)-5-(4-pyridyl)1H-imidazole, FHPI, p38 MAP Kinase Inhibitor II
Empirical Formula (Hill Notation):
C20H14FN3O
CAS Number:
Molecular Weight:
331.34
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

Assay

≥98% (HPLC)

form

solid

potency

16 nM Ki

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

pale yellow

solubility

DMSO: 50 mg/mL

shipped in

ambient

storage temp.

−20°C

InChI

1S/C20H14FN3O/c21-16-5-1-13(2-6-16)18-19(14-9-11-22-12-10-14)24-20(23-18)15-3-7-17(25)8-4-15/h1-12,23-24H

InChI key

NJNKPVPFGLGHPA-UHFFFAOYSA-N

General description

A potent, reversible, competitive, and cell-permeable inhibitor of p38 MAP kinase. Inhibits p38 phosphorylation of myelin basic protein (MBP) with no effect on the activity of the ERK or JNK MAP kinase subgroups. Also inhibits the kinase activity of p38β (Ki = 16 nM; IC50 = 350 nM) and p38 phosphorylation of activating transcription factor 2 (ATF-2; IC50 = 280 nM). Blocks LPS-induced TNF-α and interleukin biosynthesis. Reported to induce LDL receptor expression in Hep52 cells.
A potent, reversible, competitive, and cell-permeable inhibitor of p38 MAP kinase. Inhibits p38 phosphorylation of myelin basic protein (MBP) with no effect on the activity of the ERK or JNK MAP kinase subgroups. Also inhibits the kinase activity of p38β (Ki = 16 nM; IC50 = 350 nM) and p38 phosphorylation of activating transcription factor 2 (ATF-2; IC50 = 280 nM). Blocks LPS-induced TNF-α and interleukin biosynthesis. Reported to induce LDL receptor expression in Hep52 cells. A 1 mg/ml solution of SB 202190 (Cat. No. 559397) in anhydrous DMSO is also available.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
p38β
Product competes with ATP.
Reversible: yes
Target IC50: 350 nM against the kinase activity of p38β; 280 nM against p38 phosphorylation of activating transcription factor 2 (ATF-2)

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Davies, S.P., et al. 2000. Biochem. J.351, 95.
Ajizian, S.J., et al. 1999. J. Infect. Dis.179, 939.
Singh, R.P., et al. 1999. J. Biol. Chem.274, 19593.
Wang, S.W., et al. 1999. Inflamm. Res.48, 533.
Gallagher, T.F., et al. 1997. Bioorg. Med. Chem. 5, 49.
LoGrasso, P.V., et al. 1997. Biochem. 36, 10422.
Jiang, Y., et al. 1996. J. Biol. Chem. 271, 17920.
Kramer, R.M., et al. 1996. J. Biol. Chem.271, 27723.
Li, Z., et al. 1996. Biochem. Biophys. Res.Commun. 228, 334.
Lee, J.C., et al. 1994. Nature 372, 739.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

WGK

WGK 3


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