GW-5074
c-Raf1 inhibitor / Potent inhibitor of cRAF1 kinase (IC50 = 9 nM). Displays 100-fold selectivity for cRAF1 over CDK1, CDK2, c-src, ERK2, MEK, p38, Tie2, VEGFR2 and c-fm. Displays neuroprotective effects In vivo via a mechanism that is independent of MEK, ERK, and Akt signaling. Cell permeable.
Biochemicals & reagents
220904-83-6
1) Chang et al. (2005), Phorbol 12-myristate 13-acetate upregulates cyclooxygenase-2 expression in human pulmonary epithelial cells via Ras, Raf-1, ERK, and NF-kappaB, but not p38 MAPK pathways; Cell Signal., 217 299 / 2) Huang et al. (2006), Fibroblast growth factor-2 supresses oridonin-induced L929 apoptosis through extracellular signal-regulated kinase-dependent and phosphatidylinositol 3-kinase-independent pathway J. Pharmacol. Sci., 102 305 / 3) Lackey et al. (2000), The discovery of potent cRaf1 kinase inhibitors; Bioorg. Med. Chem. Lett., 10 223 / 4) Chen et al. (2004), Bradykinin B2 receptor mediates NF-kappaB activation and cyclooxygenase-2 expression via the Ras/Raf-1/ERK pathway in human airway epithelial cells; J. Immunol., 173 5219
-20°C
TARGET: Kinase -- PATHWAY: NFkappaB; Cytokine -- RESEARCH AREA: Neuroscience -- DISEASE AREA: Pain; Inflammation