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Key Documents

559388

Millipore

SB 202190

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

Sinonimo/i:

SB 202190, 4-(4-Fluorophenyl)-2-(4-hydroxyphenyl)-5-(4-pyridyl)1H-imidazole, FHPI, p38 MAP Kinase Inhibitor II

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About This Item

Formula empirica (notazione di Hill):
C20H14FN3O
Numero CAS:
152121-30-7
Peso molecolare:
331.34
Numero MDL:
MFCD00941964
Codice UNSPSC:
12352202
NACRES:
NA.77

product name

SB 202190, SB 202190, CAS 152121-30-7, is a potent, reversible, competitive inhibitor of p38. Inhibits p38 phosphorylation of myelin basic protein. Blocks the activity of p38β (Ki = 16 nM; IC₅₀ = 350 nM).

Livello qualitativo

100

Saggio

≥98% (HPLC)

Forma fisica

solid

Potenza

16 nM Ki

Produttore/marchio commerciale

Calbiochem®

Condizioni di stoccaggio

OK to freeze
protect from light

Colore

pale yellow

Solubilità

DMSO: 50 mg/mL

Condizioni di spedizione

ambient

Temperatura di conservazione

−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
NJNKPVPFGLGHPA-UHFFFAOYSA-N

Descrizione generale

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.

Azioni biochim/fisiol

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)

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

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

Altre note

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.

Note legali

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

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Certificati d'analisi (COA)

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Journal of immunology (Baltimore, Md. : 1950), 178(2), 663-670 (2007-01-05)
Dysregulated inflammation is a complication of type 2 diabetes (T2D). In this study, we show that augmented LPS-induced TNF-alpha production by resident peritoneal macrophages (PerMphi) in type 2 diabetic (db/db) mice is dependent on elevated glucose and requires p38 MAPK.
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