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Merck

559388

SB 202190

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

Synonyme(s) :

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

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A propos de cet article

Formule empirique (notation de Hill) :
C20H14FN3O
Numéro CAS:
152121-30-7
Poids moléculaire :
331.34
UNSPSC Code:
12352202
NACRES:
NA.77
MDL number:
MFCD00941964

Principaux documents

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Nom du produit

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).

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

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

Quality Level

100

Catégories apparentées

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)

Disclaimer

Toxicity: Standard Handling (A)

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 1 mg/ml solution of SB 202190 (Cat. No. 559397) in anhydrous DMSO is also available.

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.

Preparation Note

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

Legal Information

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

Classe de stockage

11 - Combustible Solids

wgk

WGK 3

Certificats d'analyse (COA)

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Consulter la Bibliothèque de documents

Christina L Sherry et al.
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.
Trine Bertelsen et al.
Annals of dermatology, 33(2), 122-130 (2021-05-04)
Interleukin (IL)-19 and IL-20 are important members of the IL-10 cytokine family, which are known to play a role in inflammatory processes. Both anti-IL-19 and -IL-20 targeting drugs have been suggested in the treatment of inflammatory diseases such as psoriasis
Muya Zhou et al.
Advanced science (Weinheim, Baden-Wurttemberg, Germany), 10(25), e2301059-e2301059 (2023-07-03)
When circulating tumor cells (CTCs) travel in circulation, they can be killed by detachment-induced anoikis and fluidic shear stress (SS)-mediated apoptosis. Circulatory treatment, which can make CTCs detached but also generate SS, can increase metastasis of cancer cells. To identify
Brooke Wang et al.
Current protocols, 4(4), e1027-e1027 (2024-04-08)
The development of patient-derived intestinal organoids represents an invaluable model for simulating the native human intestinal epithelium. These stem cell-rich cultures outperform commonly used cell lines like Caco-2 and HT29-MTX in reflecting the cellular diversity of the native intestinal epithelium
Jian-Xian Lin et al.
British journal of cancer, 123(7), 1131-1144 (2020-07-02)
Toward identifying new strategies to target gastric cancer stem-like cells (CSCs), we evaluated the function of the tumour suppressor CDK5 regulatory subunit-associated protein 3 (CDK5RAP3) in gastric CSC maintenance. We examined the expression of CDK5RAP3 and CD44 in gastric cancer
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