For research use only. Not for therapeutic Use.
Selective p38-MAPK inhibitor that targets a subset of inflammatory macrophage genes (IC50 value 2.5 nM for p38α, and no IC50 values below 5 μM, except for JNK1 (5 µM)). When used with dexamethasone, SB 706504 causes effective suppression of these genes without affecting transcription of a subset of LPS-regulated genes, including IL-1β, IL-18, and CCL5 (genes involved in the pathogenesis of COPD). Furthermore, SB 706504 reduces TNFα, GM-CSF, and IL-6 production from LPS-stimulated COPD macrophages, with less effect on IL-8 production.
KEYWORDS: SB 706504 | Supplier | p38 MAPK inhibitor | Axon Medchem | Axon 2444 | PCG | SB706504 | CAS [911110-38-8] | MAPK (p38) | Inhibitor | COPD | macrophage | inflammation | LPS | TNFα | cytokines
| Catalog Number | R024320 |
| CAS Number | 911110-38-8 |
| Molecular Formula | C24H19F3N8O |
| Purity | ≥95% |
| IUPAC Name | 1-cyano-2-[2-[[8-(2,6-difluorophenyl)-4-(4-fluoro-2-methylphenyl)-7-oxopyrido[2,3-d]pyrimidin-2-yl]amino]ethyl]guanidine |
| InChI | InChI=1S/C24H19F3N8O/c1-13-11-14(25)5-6-15(13)20-16-7-8-19(36)35(21-17(26)3-2-4-18(21)27)22(16)34-24(33-20)31-10-9-30-23(29)32-12-28/h2-8,11H,9-10H2,1H3,(H3,29,30,32)(H,31,33,34) |
| SMILES | CC1=C(C=CC(=C1)F)C2=C3C=CC(=O)N(C3=NC(=N2)NCCN=C(N)NC#N)C4=C(C=CC=C4F)F |
| Reference | L.M. Kent et al. Inhibition of lipopolysaccharide-stimulated chronic obstructive pulmonary disease macrophage inflammatory gene expression by dexamethasone and the p38 MAPK inhibitor (SB706504). J Pharmacol Exp Ther. 2009 Feb;328(2):458-68.
S.J. Tudhope et al. Different mitogen-activated protein kinase-dependent cytokine responses in cells of the monocyte lineage. J Pharmacol Exp Ther. 2008 Jan;324(1):306-12. |
