xStAx-VHLL

Pricing Availability   Qty
Cat.No. 7298 - xStAx-VHLL | Ac-Arg-Arg-Trp-Pro-Arg-[(S)-2-(4-pentenyl)alanine]-Ile-Leu-Asp-[(S)-2-(4-pentenyl)alanine]-His-Val-Arg-Arg-Val-Trp-Arg-Ahx-Ala-Leu-Ala-Pro-Tyr-Ile-Pro-NH2 (double bond covalent bridge: X-6-X-10)
Description: Selective peptide-based β-catenin degrader
Purity: ≥95% (HPLC)
Datasheet
Citations
Reviews
Literature (4)

Biological Activity

Selective peptide-based β-catenin Degrader. 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.

Technical Data

M. Wt 3231.89
Formula C154H244N48O29
Sequence RRWPRXILDXHVRRVWRALAPYIP

(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)

Storage Store at -20°C
Purity ≥95% (HPLC)
InChI Key NYZLXWJSWCBINW-OBGJTUHRSA-N
Smiles O=C([C@H](CCCNC(N)=N)NC(C)=O)N[C@@H](CCCNC(N)=N)C(N[C@@H](CC1=CNC2=C1C=CC=C2)C(N3CCC[C@H]3C(N[C@@H](CCCNC(N)=N)C(N[C@](CCC/C=C\CCC4)(C)C(N[C@@H]([C@@H](C)CC)C(N[C@@H](CC(C)C)C(N[C@@H](CC(O)=O)C(N[C@]4(C)C(N[C@@H](CC5=CN=CN5)C(N[C@@H](C(C)C)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](C(C)C)C(N[C@@H](CC6=CNC7=C6C=CC=C7)C(N[C@@H](CCCNC(N)=N)C(NCCCCCC(N[C@@H](C)C(N[C@@H](CC(C)C)C(N[C@@H](C)C(N8[C@H](C(N[C@@H](CC9=CC=C(C=C9)O)C(N[C@@H]([C@@H](C)CC)C(N%10[C@H](C(N)=O)CCC%10)=O)=O)=O)CCC8)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O

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.

Solubility Data

Solubility Soluble to 1 mg/ml in water

References

References are publications that support the biological activity of the product.

Liao et al (2020) A PROTAC peptide induces durable β-catenin degradation and suppresses Wnt-dependent intestinal cancer. Cell Discov. 6 35 PMID: 32550000


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Keywords: xStAx-VHLL, xStAx-VHLL supplier, β, beta, B, catenin, wnt, signaling, degraders, degrades, targeted, protein, degradation, TPD, PROTAC, selective, Active, Degraders, Beta-catenin, 7298, Tocris Bioscience

Citations for xStAx-VHLL

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Targeted Protein Degradation

Targeted Protein Degradation Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:

  • Active Degraders
  • Degrader Building Blocks
  • Custom Degrader Services
  • UPS Proteins and Assays
  • Assays for Protein Degradation
Epigenetics

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

Epigenetics in Cancer

Epigenetics in Cancer Poster

Adapted from the 2015 Cancer Product Guide Edition 3, this poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.

Targeted Protein Degradation

Targeted Protein Degradation Poster

Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia