SP 100030

Biological Activity

SP 100030 is a potent dual inhibitor of NF-κB and AP-1 transcriptional activity (IC₅₀ = 50 nM). Blocks production of IL-2, IL-8 and TNF-α from Jurkat T cells. Inhibits cytokine production selectively in T cells; exhibits minimal inhibition of cytokine production in other cell types. Decreases arthritic severity in a mouse model of collagen-induced arthritis. Also ameliorates muscle wasting in a rat model of cancer cachexia.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. The effect of a T cell-specific NF-κB inhibitor on in vitro cytokine production and collagen-induced arthritis
   Gerlag et al.
   J.Immunol., 2000;165:1652
2. 2-Chloro-4-(trifluoromethyl)pyrimidine-5-N-(3',5'- bis(trifluoromethyl)phenyl)-carboxamide: a potent inhibitor of NF-κB- and AP-1-mediated gene expression identified using solution-phase combinatorial ch
   Sullivan et al.
   J.Med.Chem., 1998;41:413
3. The AP-1/NF-κB double inhibitor SP100030 can revert muscle wasting during experimental cancer cachexia.
   Moore-Carrasco et al.
   Int.J.Oncol., 2007;30:1239

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