N-(4-Trifluoromethylphenyl)-2-cyano-3-hydroxycrotoamide White solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. Leflunomide metabolite that blocks TNF-dependent NF-kB activation and gene expression. Inhibits the activity of dihydroorotate dehydrogenase (DHO-DH; IC50 = 220 nM). Reported to reduce IFN-g-induced expression of iNOS in L929 fibroblasts. Inhibits IL-1b-induced activation of COX-2 and PGE2 synthesis (IC50 = 130 nM) in A549 cells. Also inhibits the IL-2-induced tyrosine phosphorylation of JAK1 and JAK3. Purity: ≥97% by HPLC. CAS 108605-62-5. Ref.: Jankovic, V., et al. 2000. Cell Immunol. 199, 73. Hamilton, L.C., et al. 1999. Br. J. Pharmacol. 127, 1589. Manna, S.K., and Aggarwal, B.B. 1999. J. Immunol. 162, 2095. Elder, R.T., et al. 1997. J. Immunol. 159, 22. Xu, X., et al. 1996. Biochem. Pharmacol. 52, 527. Xu, X., et al. 1995. J. Biol. Chem. 270, 12398. Mattar, T., et al. 1993. FEBS Lett. 334, 161.
R: 40; S: 22-36 |
