SP-100030 

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

SP100030 (10 mg/kg/day; i.p.; day 21 to day 34) significantly decreased arthritis severity^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

437.65

Solid

C₁₄H₅ClF₉N₃O

154563-54-9

FC(F)(F)C1=CC(C(F)(F)F)=CC(NC(C2=CN=C(Cl)N=C2C(F)(F)F)=O)=C1

Room temperature in continental US; may vary elsewhere.

• [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  [Content Brief]

  [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.  [Content Brief]