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].

Research Areas >> Inflammation/Immunology

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]. Animal Model: Six- to 8-wk-old male DBA/1J mice (immunized with type II collagen)[2] Dosage: 10 mg/kg Administration: I.p.; daily, starting at day 21 to the end of the study on day 34 Result: Significantly decreased arthritis scores compared with controls; Histologic evaluation of the paws from mice treated from day 20 to 34 showed a trend toward decreased inflammation.

[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;41(4):413-419.

[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.