SB 239063

Modify Date: 2024-01-11 17:39:50

SB 239063 Structure
SB 239063 structure
Common Name SB 239063
CAS Number 193551-21-2 Molecular Weight 368.40500
Density 1.35g/cm3 Boiling Point 594.8ºC at 760 mmHg
Molecular Formula C20H21FN4O2 Melting Point N/A
MSDS USA Flash Point 313.5ºC

 Use of SB 239063


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.

 Names

Name 4-[4-(4-fluorophenyl)-5-(2-methoxypyrimidin-4-yl)imidazol-1-yl]cyclohexan-1-ol
Synonym More Synonyms

 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
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.

 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

 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

~64%

SB 239063 Structure

SB 239063

CAS#:193551-21-2

Literature: SmithKline Beecham Corporation Patent: US6329526 B1, 2001 ;

 Precursor & DownStream

Precursor  1

DownStream  0

 Synonyms

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