Biochem/physiol Actions

Primary TargetNEMO-binding peptide

Reversible: yes

Cell permeable: yes

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 TNFA-stimulated NF-κB activity (IC₅₀ ~ 50 µM in HCT116 cells). Acts by interfering with the formation of active IKK complex and thereby prevents IκBA 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).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Hong, S., et al. 2012. Mol. Pharm.9, 1310.Kim, D., et al. 2006. Exp. Cell Res.312, 1277.

Packaging

5 mg in Glass bottle

Packaged under inert gas

Yes

Sequence

Ac-YGRRARRRARRTALDWSWLQTE-NH₂

Warning

Toxicity: Standard Handling (A)