The p38 MAPK family consists of highly conserved proline-directed serine-threonine protein kinases that are activated in response to a number many growth factors, cytokines, and chemotactic substances, such as vascular endothelial growth factor (VEGF), fibroblast growth factor (FGF), PDGF, TNF, interleukins, lipopolysaccharide (LPS) and formyl-methionyl-leucyl-phenylalanine (fMLP). It is well known that p38 is involved in inflammation, apoptosis, cardiomyocyte hypertrophy and cell differentiation.
The p38 MAPK family is composed of four proteins: p38α (encoded by the gene Mapk14), p38β (Mapk11), p38γ (Mapk12), and p38δ (Mapk13). Their coding genes have a distinct tissue distribution and they appear differentially expressed, being Mapk14 the most highly expressed. p38 MAPKs are substrates for three MAP2K (MKK6, MKK3, and MKK4). The contribution of each of these MAP2K to p38 MAPKs activation depends on the stimulus and the cell type. The MAP3Ks that lead to p38 MAPKs activation are ASK1, DLK1, TAK1, TAO1, TAO2, TPL2, MLK3, MEKK3, MEKK4, and ZAK1.
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SKF-86002 is a potent inhibitor of p38 MAPK with IC50 of 0.5-1 uM, inhibits LPS-induced IL-1 and TNF-α production in human monocyte with IC50 of 1 uM; inhibits prostaglandin H2 (PGH2) synthase activity (IC50=120 uM) as well as prostanoid production by rat basophilic leukemia (RBL-1) cells (IC50=70 uM); blocks superoxide anion production in response to FMLP and reduces adhesion and chemotaxis in response to PAF or FMLP in human neutrophils; also inhibits 5-lipoxygenase- and cyclooxygenase-mediated arachidonic acid metabolism in RBL-1 cells (IC50=10 and 100 uM respectively), shows anti-inflammatory in vivo.
A potent, selective, orally active p38 MAPK inhibitor that inhibits the production of TNF-α and IL-1β by LPS-stimulated human PBMCs with IC50 of 3 and 11 nM, respectively; inhibits p38α from purified LPS-activated human monocytes with IC50 of 30 nM, less potent for p38β; also inhibits Src (IC50=5 uM), p65 Lck and no activity against other MAPKs and serine-threonine kinases; inhibits TNF-alpha production in LPS-injected mice.
A selective p38 MAPK inhibitor; inhibits IL-1 beta induction of p38 MAPK in primary human chondrocytes with IC50 of 1 uM; inhibits LPS-stimulated serum levels of TNFalpha in normal rats with mean ED50 of 3.99 mg/kg.
A potent p38 MAPK inhibitor with IC50 of 20 nM; inhibits the phosphorylation of proteins downstream of p38α MAPK such as MAPKAPK2 and HSP27 during cardiogenesis, and increases ATF-2 and MEF2C during cardiac differentiation.
A potent, selective p38 MAPK inhibitor with IC50 of 89 nM; displays >100-fold selectivity over ERK, PKA, PKCα; prevent p38 phosphorylation while promotes the phosphorylation of the pro-survival SAPK/JNK and ERK;
MW-150 is a novel potent, selective, CNS penetrant and orally active inhibitor of p38α MAPK with Ki of 101 nM; effectively suppresses hippocampal-dependent associative and spatial memory deficits in synaptic dysfunction mouse models; also can selectively modulate neuroinflammatory responses associated with pathology progression.
MW-150 hydrochloride is a novel potent, selective, CNS penetrant and orally active inhibitor of p38α MAPK with Ki of 101 nM; effectively suppresses hippocampal-dependent associative and spatial memory deficits in synaptic dysfunction mouse models; also can selectively modulate neuroinflammatory responses associated with pathology progression.
p38 MAPK-IN-4 is a potent and selective inhibitor of p38 MAPK with IC50 of 68 nM for p38α, inhibits LPS-induced TNFα release in THP-1 cells with IC50 of 187 nM; displays no signigicant activity against a panel of 54 tyrosine kinases and serine/threonine kinases; dose-dependently inhibits TNFα production with an ED50 of 0.5 mg/kg in rat-LPS induced TNFα model, dose-dependently inhibits arthritis progression with ED50 <1 mg/kg, demonstrates a superior efficacy of 4 versus other clinically tested reference compounds like BIRB-796 and VX-745.
A potent, selective, orally active p38α MAPK inhibitor with IC50 of 7.1 nM; displays >20-fold selectvity over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1; inhibits LPS-stimulated release of TNF-alpha from THP-1 with IC50 of 48 nM; exerts significant efficacy in rat adjuvant-induced arthritis model.
SB 203580 HCl
A specific p38 MAPK inhibitor with IC50 of 0.6 uM; shows selectivity over JNK, p42 MAPK, p90 S6K, p70 S6K, PKA, etc.; suppresses the activation of MAPKAP kinase-2 and prevents the phosphorylation of HSP27 in response to interleukin-1, cellular stresses and bacterial endotoxin in vivo.
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