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SB 706504
- PCG
- Soluble in DMSO
- MF: C24H19F3N8O
- MW: 492.46
Description
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.
More Information
| Parent CAS No. | 911110-38-8 |
|---|---|
| Chemical Name | N-cyano-N'-[2-[[8-(2,6-difluorophenyl)-4-(4-fluoro-2-methylphenyl)-7,8-dihydro-7-oxopyrido[2,3-d]pyrimidin-2-yl]amino]ethyl]-guanidine |
| SMILES | N(C#N)C(=N)NCCNC1=NC(C2=CC=C(F)C=C2C)=C2C=CC(=O)N(C3=C(F)C=CC=C3F)C2=N1 |
| MFCD | N.A. |
| 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) |
| InChiKey | ZQFBVJBAWLZLOM-UHFFFAOYSA-N |
| CID | 11853799 |
| Short Description | p38 MAPK inhibitor |
References
- 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.
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