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).

Legal Information

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

Other Notes

Steel, R., et al. 2012. ACS Med Chem Lett.3, 407.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Physical form

Supplied as a trifluoroacetate salt.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Sequence

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

Warning

Toxicity: Standard Handling (A)