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Description

A cell-permeable cytoplasmic transduction peptide (CTP, YGRRARRRARR) fused to the NEMO binding domain peptide (NBD, TALDWSWLQTE) that acts as a potent inhibitor of TNF&alpha,-stimulated NF-&kappa,B activity (IC50 ~ 50 microM in HCT116 cells). Acts by interfering with the formation of active IKK complex and thereby prevents I&kappa,B&alpha, phosphorylation and its subsequent proteasomal degradation. Also blocks LPS-mediated increase in inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) activities. Colon-targeted capsules containing CTP-NBD are shown to reduce 2,4,6-trinitrobenzenesulfonic acid (TNBS)-induced colitis in rodent models (4.5 mg/kg/,p.o.) in vivo and diminish activities of myeloperoxidase and several inflammatory mediators. Antennapedia fused NBD cell-permeable peptide is also available (>Cat. No. 480025).