Description
General description
A 14-mer peptide (LQLDEETGEFLPIQ) conjugated to cell-penetrating trans-activating transcriptional activator (TAT) sequence (YGRKKRRQRRRLQ) that targets the nuclear factor (erythroid-derived 2)-like 2 (Nrf2) binding site on Kelch-like ECH-associated protein 1 (Keap1). Competitively disrupts Nrf2-Keap1 interaction and stabilizes cytosolic Nrf2, and promotes its nuclear translocation and binding to the antioxidant response element (ARE). Exhibits anti-inflammatory properties and increases heme-oxygenase-1 gene expression (~75 µM). Also shown to suppress LPS-induced TNF-α secretion in THP-1 monocytes (~ 37.5 µM).
Packaging
Packaged under inert gas
Physical form
Supplied as a trifluoroacetate salt.
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
H-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg~Leu-Gln-Leu-Asp-Glu-Glu-Thr-Gly-Glu-Phe-Leu-Pro-Ile-Gln-OH
Steel, R., et al. 2012. ACS Med Chem Lett.3, 407.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
