For research use only. Not for therapeutic Use.
SP-100030 is a potent NF-κB and activator protein-1 (AP-1) double inhibitor (IC50s=50 and 50 nM, respectively). SP-100030 inhibits IL-2, IL-8, and TNF-alpha production in Jurkat and other T cell lines. SP-100030 decreases murine collagen-induced arthritis (CIA)[1][2].
SP-100030 blocks the production of IL-2 and IL-8 in Jurkat T-cells at the same concentrations as seen in the luciferase assay (IC50≈30 nM)[1].
ELISA and RT-PCR confirmed that IL-2, IL-8, and TNF-alpha production by activated Jurkat and other T cell lines were inhibited by SP100030[2].
SP100030 (10 mg/kg/day; i.p.; day 21 to day 34) significantly decreased arthritis severity[2].
| Catalog Number | I011161 |
| CAS Number | 154563-54-9 |
| Synonyms | N-[3,5-bis(trifluoromethyl)phenyl]-2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxamide |
| Molecular Formula | C14H5ClF9N3O |
| Purity | ≥95% |
| InChI | InChI=1S/C14H5ClF9N3O/c15-11-25-4-8(9(27-11)14(22,23)24)10(28)26-7-2-5(12(16,17)18)1-6(3-7)13(19,20)21/h1-4H,(H,26,28) |
| InChIKey | GHMKQBWHPQMXSH-UHFFFAOYSA-N |
| SMILES | C1=C(C=C(C=C1C(F)(F)F)NC(=O)C2=CN=C(N=C2C(F)(F)F)Cl)C(F)(F)F |
| Reference | [1]. Sullivan RW, et al. 2-Chloro-4-(trifluoromethyl)pyrimidine-5-N-(3′,5′- bis(trifluoromethyl)phenyl)-carboxamide: a potent inhibitor of NF-kappa B- and AP-1-mediated gene expression identified using solution-phase combinatorial chemistry. J Med Chem. 1998;4 [2]. Gerlag DM, et al. The effect of a T cell-specific NF-kappa B inhibitor on in vitro cytokine production and collagen-induced arthritis. J Immunol. 2000;165(3):1652-1658. |
