Dvl-PDZ Domain Inhibitor, Peptide Pen-N3

A 22-amino acid PDZ domain-binding carboxamide toward Dvl (dishevelled) family proteins is fused at the N-terminal with a 16-mer antennapedia homeodomain-derived cell-permeable acetamide to facilitate its use in cellular studies. Shown to selectively inhibit the upregulation of cellular β-catenin accumulation and transcription activity upon Wnt3a stimulation (IC₅₀ = 11 µM) or Dvl1/2/3 overexpression in HEK293 cultures, but not the Wnt3a- or Dvl1/2/3-independent, constitutively active Wnt pathway signaling in the APC-mutant HCT-15 colon cancer cells. Unlike Box5, the PDZ-interacting sequence in Pen-N3, originally identified via a random phage display screening, is not derived from Wnt or other known cellular proteins.

Packaged under inert gas

Supplied as a trifluoroacetate salt

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Ac-Arg-Gln-Ile-Lys-Ile-Trp-Phe-Gln-Asn-Arg-Arg-Met-Lys-Trp-Lys-Lys-Gly-Gly-Gly-Glu-Ile-Val-Leu-Trp-Ser-Asp-Ile-Pro-NH₂

Zhang, Y., et al. 2009. Nat. Chem. Biol.5, 217.

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

Toxicity: Standard Handling (A)