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Description

A cell-permeable, non-toxic, conformationally restricted pyrimidinecarboxamide compound that acts as a potent, reversible T-cell specific inhibitor of both AP-1 and NF-kappaB transcriptional activation (IC50 = 50 nM). Reduces DNA binding activity of NF-kappaB and downregulates NF-kappaB driven cytokine gene expression. Displays only trivial inhibitory effect against cytokine induction in a variety of other cells. Exhibits anti-inflammatory activity in a murine model of collagen-induced arthritis (~ 10 mg/kg/d, i.p.) and suppresses the expansion of AH-130 Yoshida ascites hepatoma in rats (~ 5 mg/kg/d, i.p.).Please note that the molecular weight for this compound is batch-specific due to variable water content., A cell-permeable, conformationally restricted pyrimidinecarboxamide compound that is reported to inhibit against the activation of AP-1- & NF-kappaB-, but not &beta-actin-, mediated transcriptions (IC50 = 50 nM in Jurkat-based reporter assays, 0.5 h drug pretreatment prior to 5 h stimulation with 1 µ,g/mL PHA/526511 & 50 ng/mL PMA/500582 & 524400) and target genes expressions, including IL-2, IL-8, TNF-alpha, in 6 T cell cultures (by >85% at 3 µ,M), while exhibiting little inhibitory potency against cytokine inductions in 10 non-T cell cultures (by <5% at 10 µ,M), including endothelial, epithelial, fibroblast, monocytic, and osteoblast cultures. Intraperitoneal injection is shown to display in vivo anti-inflammatory efficacy in a murine model of collagen-induced arthritis (10 mg/kg/d) and a rodent model of Ova-induced asthma response (20 mg/kg/d). Dual AP-1 & NF-kappaB inhibition via daily SP100030 subcutaneous injection is also reported to suppress AH-130 Yoshida ascites hepatoma tumor expansion in rats in vivo (5 mg/kg/d).