Potent dual inhibitor of NF-κ
B 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.
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The effect of a T cell-specific NF-κB inhibitor on in vitro cytokine production and collagen-induced arthritis
Gerlag et al.
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.
The AP-1/NF-κB double inhibitor SP100030 can revert muscle wasting during experimental cancer cachexia.
Moore-Carrasco et al.