Drug intelligence / Profile preview

SB 239063

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

SB 239063 is a **potent, cell-permeable, orally active, and highly selective small molecule inhibitor of p38 mitogen-activated protein kinase (MAPK)**, specifically showing high affinity for p38α and p38β isoforms (IC50 = 44 nM), with negligible effect on p38γ and p38δ (IC50 > 100 μM)[1][4][7]. It demonstrates over 220-fold selectivity for p38 over other related kinases like ERK and JNK1[1][8]. SB 239063 has been shown to reduce inflammatory cytokine production, such as interleukin-1 (IL-1) and tumor necrosis factor-alpha (TNF-α) in immune cells, and to provide neuroprotection in models of cerebral ischemia and neuroinflammation[4][6][7][9][10]. The compound has also demonstrated efficacy in reducing infarct size and neurological deficits in animal models of stroke and has been studied for its ability to prevent hepatic insulin resistance[3][6][7].

Other names
trans-1-(4-hydroxycyclohexyl)-4-(4-fluorophenyl)-5-(2-methoxypyrimidin-4-yl)imidazoleCyclohexanol, 4-(4-(4-fluorophenyl)-5-(2-methoxy-4-pyrimidinyl)-1H-imidazol-1-yl)-trans-p38 MAP Kinase Inhibitor XVp-38 MAP Kinase Inhibitor XVp 38 MAP Kinase Inhibitor XV
02

Targets

MAPK11 (p38 beta mitogen-activated protein kinase)MAPK14 (p38 mitogen-activated protein kinase alpha)

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