Description
General 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 TNFα-stimulated NF-κB activity (IC₅₀ ~ 50 µM in HCT116 cells). Acts by interfering with the formation of active IKK complex and thereby prevents IκBα 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 ).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
NEMO-binding peptide
Reversible: yes
Packaging
Packaged under inert gas
Yes
Other Notes
Ac-YGRRARRRARRTALDWSWLQTE-NH₂
Hong, S., et al. 2012. Mol. Pharm.9, 1310.
Kim, D., et al. 2006. Exp. Cell Res.312, 1277.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
