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About This Item
Empirical Formula (Hill Notation):
C20H14FN3O
CAS Number:
Molecular Weight:
331.34
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
liquid
Quality level:
Storage condition:
OK to freeze, protect from light
Quality Level
assay
≥98% (HPLC)
form
liquid
potency
16 nM IC50, 16 nM Ki
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
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
P38β
Product competes with ATP.
Reversible: yes
Target Ki: 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.
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)
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Storage Class
10 - Combustible liquids
wgk
WGK 1
flash_point_f
188.6 °F - closed cup - (Dimethylsulfoxide)
flash_point_c
87 °C - closed cup - (Dimethylsulfoxide)
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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Matriptase drives dissemination of ovarian cancer spheroids by a PAR-2/PI3K/Akt/MMP9 signaling axis.
Nisha R Pawar et al.
The Journal of cell biology, 222(11) (2023-09-22)
The transmembrane serine protease matriptase is a key regulator of both barrier-disruptive and protective epithelial cell-cell interactions. Elevated matriptase is a consistent feature of epithelial ovarian cancers (OvCa), where multicellular spheroids shed from the primary tumor into the peritoneal cavity