559388

SB 202190

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

• Szinonimák: SB 202190, 4-(4-Fluorophenyl)-2-(4-hydroxyphenyl)-5-(4-pyridyl)1H-imidazole, FHPI, p38 MAP Kinase Inhibitor II
• Tapasztalati képlet (Hill-képlet): C₂₀H₁₄FN₃O
• CAS-szám: 152121-30-7
• Molekulatömeg: 331.34
• MDL-szám: MFCD00941964
• UNSPSC kód: 12352202
• NACRES: NA.77

Tulajdonságok

• Terméknév: 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).
• Minőségi szint: 100
• Teszt: ≥98% (HPLC)
• Forma: solid
• hatékonyság: 16 nM K_i
• gyártó/kereskedő neve: Calbiochem^®
• tárolási körülmény: OK to freeze; protect from light
• szín: pale yellow
• oldhatóság: DMSO: 50 mg/mL
• kiszállítva: ambient
• tárolási hőmérséklet: −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
• Nemzetközi kémiai azonosító kulcs: NJNKPVPFGLGHPA-UHFFFAOYSA-N

Leírás

Általános leírás

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 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.

Biokémiai/fiziológiai hatások

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)

Figyelmeztetés

Toxicity: Standard Handling (A)

Feloldás

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

Egyéb megjegyzések

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.

Jogi információk

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

Biztonsági adatok

• Tárolási osztály kódja: 11 - Combustible Solids
• WGK: WGK 3