SB239063

ALX-270-351

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p38 inhibitor

A potent, cell permeable inhibitor of p38 MAP kinase (IC₅₀=44nM for recombinant purified human p38α). Inhibits IL-1 and TNF-α production in LPS-stimulated human peripheral blood monocytes (IC₅₀=120nM and 350nM, 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, reduces myocardial reperfusion injury via inhibition of endothelial adhesion molecule expression and blockade of polymorphonuclear (PMN) accumulation.

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Product Details

Alternative Name	trans-1-(4-Hydroxycyclohexyl)-4-(fluorophenyl)-5-(2-methoxypyrimidin-4-yl) imidazole
Appearance	White to off-white solid.
CAS	193551-21-2
Couple Target	p38
Couple Type	Inhibitor
Formula	C₂₀H₂₁FN₄O₂
Identity	Identity determined by 1H-NMR.
MW	368.4
Purity	≥97% (HPLC)
Solubility	Soluble in DMSO, 100% ethanol or dichlormethane (may require slight warming).

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended.
Handling	Protect from light. Packaged under inert gas.
Long Term Storage	-20°C
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

Apelin-13 protects neurovascular unit against ischemic injuries through the effects of vascular endothelial growth factor: C. Huang, et al.; Neuropeptides 60, 67 (2016), Application(s): Investigating possible signal transduction pathways in rat MCAO model, Abstract
Human CD1c⁺ myeloid dendritic cells acquire a high level of retinoic acid-producing capacity in response to vitamin D₃: Sato, T., Kitawaki, T., et al.; J. Immunol. 191, 3152 (2013), Abstract
Activation of p38 MAPK by reactive oxygen species is essential in a rat model of stress-induced gastric mucosal injury: Y.T. Jia, et al.; J. Immunol. 179, 7808 (2007), Abstract
p38 MAPK inhibition reduces myocardial reperfusion injury via inhibition of endothelial adhesion molecule expression and blockade of PMN accumulation: F. Gao, et al.; Cardiovasc. Res. 53, 414 (2002), Abstract
Sustained activation of p38 mitogen-activated protein kinase contributes to the vascular response to injury: H. Ju, et al.; J. Pharmacol. Exp. Ther. 301, 15 (2002), Abstract
The selective p38 inhibitor SB-239063 protects primary neurons from mild to moderate excitotoxic injury: J.J. Legos, et al.; Eur. J. Pharmacol. 447, 37 (2002), Abstract
SB 239063, a second-generation p38 mitogen-activated protein kinase inhibitor, reduces brain injury and neurological deficits in cerebral focal ischemia: F.C. Barone, et al.; J. Pharmacol. Exp. Ther. 296, 312 (2001), Abstract — Full Text
SB-239063, a potent and selective inhibitor of p38 map kinase: preclinical pharmacokinetics and species-specific reversible isomerization: K.W. Ward, et al.; Pharm. Res. 18, 1336 (2001), Abstract
SB 239063, a potent p38 MAP kinase inhibitor, reduces inflammatory cytokine production, airways eosinophil infiltration, and persistence: D.C. Underwood, et al.; J. Pharmacol. Exp. Ther. 293, 281 (2000), Abstract — Full Text

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SB239063

ALX-270-351

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Handling & Storage

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