559388

SB 202190

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

• Synonyma: SB 202190, 4-(4-Fluorophenyl)-2-(4-hydroxyphenyl)-5-(4-pyridyl)1H-imidazole, FHPI, p38 MAP Kinase Inhibitor II
• Empirický vzorec (Hillův zápis): C₂₀H₁₄FN₃O
• Číslo CAS: 152121-30-7
• Molekulová hmotnost: 331.34
• UNSPSC Code: 12352202
• NACRES: NA.77
• MDL number: MFCD00941964
• Assay: ≥98% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Vlastnosti

• Název produktu: 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 (K_i = 16 nM; IC₅₀ = 350 nM).
• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: solid
• potency: 16 nM K_i
• 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
• SMILES string: Fc1ccc(cc1)C2=C(NC(=C4C=CC(=O)C=C4)N2)c3ccncc3
• 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

Popis

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 (K_i = 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)

Preparation Note

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

Disclaimer

Toxicity: Standard Handling (A)

Bezpečnostní informace

• Skladovací třída: 11 - Combustible Solids