559397

SB 202190

InSolution, ≥98%, p38 MAP kinase inhibitor

• Synonym(e): InSolution SB 202190, InSolution p38 MAP Kinase Inhibitor II
• Empirische Formel (Hill-System): C₂₀H₁₄FN₃O
• CAS-Nummer: 152121-30-7
• Molekulargewicht: 331.34
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD00941964
• Assay: ≥98% (HPLC)
• Form: liquid
• Quality level: 100
• Storage condition: OK to freeze, protect from light

Eigenschaften

• Quality Level: 100
• assay: ≥98% (HPLC)
• form: liquid
• potency: 16 nM IC₅₀, 16 nM K_i
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• shipped in: wet ice
• 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

Beschreibung

General description

A potent 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 (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 block LDL expression in Hep52 cells.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
P38β

Product competes with ATP.

Reversible: yes

Target K_i: 350 nM against the kinase activity of p38β; 280 nM against p38 phosphorylation of activating transcription factor 2 (ATF-2)

Packaging

Packaged under inert gas

Please refer to vial label for lot-specific concentration.

Physical form

A 1 mg/ml solution of SB 202190 (Cat. No. 559388) in anhydrous DMSO.

Preparation Note

Following initial thaw, aliquot and freeze (-20°C).

Other Notes

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.
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, L.C., et al. 1994. Nature372, 739.

Legal Information

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

Disclaimer

Toxicity: Irritant (B)

Sicherheitshinweise

• Lagerklasse: 10 - Combustible liquids
• wgk: WGK 1
• flash_point_f: 188.6 °F - closed cup - (Dimethylsulfoxide)
• flash_point_c: 87 °C - closed cup - (Dimethylsulfoxide)