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SB 239063

Names

[ CAS No. ]:
193551-21-2

[ Name ]:
SB 239063

[Synonym ]:
trans-1-(4-Hydroxycyclohexyl)-4-(4-fluorophenyl)-5-(2-methoxypyridimidin-4-yl)imidazole
Kinome_3168
Tocris-1962
SB 239063

Biological Activity

[Description]:

SB 239063 is a potent and selective p38 MAPK inhibitor (IC50 = 44 nM for p38α). SB 239063 displays > 220-fold selectivity over ERK, JNK1 and other kinases; ~ 3-fold more selective than SB 203580. IC50 value: 44 nM ( p38α)Target: p38 MAPKSB 239063 reduces inflammatory cytokine production and is neuroprotective following oral administration in vivo.

[Related Catalog]:

Signaling Pathways >> MAPK/ERK Pathway >> p38 MAPK
Research Areas >> Inflammation/Immunology

[References]

[1]. Bison S, et al. Effect of the p38 MAPK inhibitor SB-239063 on Lipopolysaccharide-induced psychomotor retardation and peripheral biomarker alterations in rats.Eur J Pharmacol. 2011 Jul 1;661(1-3):49-56. Epub 2011 Apr 27.

[2]. Ward KW, et al. SB-239063, a potent and selective inhibitor of p38 map kinase: preclinical pharmacokinetics and species-specific reversible isomerization.Pharm Res. 2001 Sep;18(9):1336-44.

[3]. Barone FC, et al. SB 239063, a second-generation p38 mitogen-activated protein kinase inhibitor, reduces brain injury and neurological deficits in cerebral focal ischemia.J Pharmacol Exp Ther. 2001 Feb;296(2):312-21.

[4]. Underwood et al (2000) SB 239063, a potent p38 MAP kinase inhibitor, reduces inflammatory cytokine production, airways eosinophil infiltration, and persistence. J.Pharmacol.Exp.Ther. 293 281.

[5]. Legos et al (2002) The selective p38 inhibitor SB-239063 protects primary neurons from mild to moderate excitotoxic injury. Eur.J.Pharmacol. 447 37.

[6]. Matthew Huentelman, et al. Methods of treating memory loss and enhancing memory performance. US 20120245188 A1.


[Related Small Molecules]

SB203580 | SB202190 (FHPI) | Doramapimod (BIRB 796) | LY2228820 | Losmapimod | PD 169316 | Talmapimod | Tat-NR2B9c | Dehydrocorydaline chloride | TAK-715 | VX 702 | VX-745 | SKF 86002 | Acumapimod | PH-797804

Chemical & Physical Properties

[ Density]:
1.35g/cm3

[ Boiling Point ]:
594.8ºC at 760 mmHg

[ Molecular Formula ]:
C20H21FN4O2

[ Molecular Weight ]:
368.40500

[ Flash Point ]:
313.5ºC

[ Exact Mass ]:
368.16500

[ PSA ]:
73.06000

[ LogP ]:
3.63080

[ Vapour Pressure ]:
5.42E-15mmHg at 25°C

[ Index of Refraction ]:
1.655

[ Storage condition ]:
-20°C

MSDS

Click to get detail MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

[ RTECS ]:
GV9458000

Synthetic Route

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Precursor & DownStream

Precursor

DownStream

Related Compounds