Biological ActivityxStAx-VHLL is a selective peptide-based β-catenin Degrader (PROTAC®). Comprises a β-catenin-targeted stapled peptide, xStAx, linked to a VHL-binding peptide. Reduces β-catenin levels in HEK293T cells and colorectal cancer cell lines. Selectively degrades β-catenin over other Wnt signaling pathway components. Inhibits tumor growth in APCmin/+ mice, with constitutively active Wnt signaling, and reduces survival of patient-derived colorectal cancer cell organoids.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
(Modifications: Arg-1 = N-terminal Ac, X = (S)-2-(4-pentenyl)alanine, X-6 and X-10 stapled together with a double bond, Arg-17 = Arg-Ahx, Pro-24 = C-terminal amide)
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Complete Your Research
A PROTAC peptide induces durable β-catenin degradation and suppresses Wnt-dependent intestinal cancer.
Liao et al.
Cell Discov., 2020;6:35
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