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Merck

559404

SB 239063

A potent, cell-permeable, reversible, and ATP-competitive inhibitor of the α- and β-isoforms (IC50 = 44 nM), but not the γ- or δ-isoform (IC50 > 100 µM), of MAP kinase p38.

Synonym(s):

SB 239063, trans-1-(4-Hydroxycyclohexyl)-4-(4-fluorophenyl)-5-(2-methoxypyrimidin-4-yl)imidazole, p38 MAP Kinase Inhibitor XV

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About This Item

Empirical Formula (Hill Notation):
C20H21FN4O2
CAS Number:
193551-21-2
Molecular Weight:
368.40
UNSPSC Code:
12352200
MDL number:
MFCD03792786

Product Name

SB 239063, A potent, cell-permeable, reversible, and ATP-competitive inhibitor of the α- and β-isoforms (IC50 = 44 nM), but not the γ- or δ-isoform (IC50 > 100 µM), of MAP kinase p38.

InChI key

ZQUSFAUAYSEREK-UHFFFAOYSA-N

InChI

1S/C20H21FN4O2/c1-27-20-22-11-10-17(24-20)19-18(13-2-4-14(21)5-3-13)23-12-25(19)15-6-8-16(26)9-7-15/h2-5,10-12,15-16,26H,6-9H2,1H3

assay

≥97% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white

solubility

DMSO: 0.5-1 mg/mL

shipped in

ambient

storage temp.

−20°C

Quality Level

100

Biochem/physiol Actions

Primary Target
MAPKp38α & β
Product competes with ATP.
Reversible: yes
Cell permeable: yes
Target IC50: 44 nM against of the α- and β-isoforms of MAP kinase p38; <100 µM against the γ- or δ-isoform of MAP kinase p38

Disclaimer

Toxicity: Standard Handling (A)

General description

A potent, cell-permeable, reversible, and ATP-competitive inhibitor of the α and β isoforms (IC50 = 44 nM), but not the γ or δ isoforms (IC50 >100 µM) of p38 MAP kinase. Inhibits IL-1 and TNF-a production in LPS-stimulated human peripheral blood monocytes (IC50 = 120 nM and 350 nM, respectively). Reported to protect against mild excitotoxic neuronal injury caused by NMDA and provides substantial protection against cell death induced by either oxygen glucose deprivation (OGD) or magnesium deprivation in cultured neurons. Also reported to reduce myocardial reperfusion injury via inhibition of endothelial adhesion molecule expression and blockade of polymorphonuclear (PMN) accumulation.

Other Notes

Gao, F., et al. 2002. Cardiovasc. Res.53, 414.
Ju, H., et al. 2002. J. Pharmacol. Exp. Ther.301, 15.
Legos, J.J., et al. 2002. Eur. J. Pharmacol.447, 37.
Barone, F.C., et al. 2001. J. Pharmacol. Exp. Ther.296, 312.
Ward, K.W., et al. 2001. Pharm. Res.18, 1336.
Underwood, D.C., et al. 2000. J. Pharmacol. Exp. Ther.293, 281.
Underwood, D.C., et al. 2000. Am. J. Physiol. Lung Cell Mol. Physiol.279, L895.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
May require slight warming to achieve complete solubilization.

Legal Information

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

Storage Class

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

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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