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Submit ReviewxStAx-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.
β-catenin antibodies validated for Simple Western™ (automated Western) instruments and Western Blot also available: Catalog # AF1329 and NBP1-54467.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
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 | IAIGOXKADOABIF-BDNJFVESSA-N |
Smiles | O=C(N[C@H](C(N[C@H](C(N1CCC[C@H]1C(N[C@H](C(N[C@](C)(C(N[C@H](C(N[C@H](C(N[C@H]2CC(O)=O)=O)CC(C)C)=O)[C@H](CC)C)=O)CCC/C=C\CCC[C@@](C)(C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(NCCCCCC(N[C@H](C(N[C@H](C(N[C@H](C(N3[C@@H](CCC3)C(N[C@H](C(N[C@H](C(N4[C@@H](CCC4)C(N)=O)=O)[C@H](CC)C)=O)CC5=CC=C(O)C=C5)=O)=O)C)=O)CC(C)C)=O)C)=O)=O)CCCNC(N)=N)=O)CC6=CNC7=C6C=CC=C7)=O)C(C)C)=O)CCCNC(N)=N)=O)CCCNC(N)=N)=O)C(C)C)=O)CC8=CN=CN8)=O)NC2=O)=O)CCCNC(N)=N)=O)=O)CC9=CNC%10=C9C=CC=C%10)=O)CCCNC(N)=N)[C@@H](NC(C)=O)CCCNC(N)=N.O=C(N[C@H](C(N[C@H](C(N%11CCC[C@H]%11C(N[C@H](C(N[C@](C)(C(N[C@H](C(N[C@H](C(N[C@H]%12CC(O)=O)=O)CC(C)C)=O)[C@H](CC)C)=O)CCC/C=C/CCC[C@@](C)(C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(NCCCCCC(N[C@H](C(N[C@H](C(N[C@H](C(N%13[C@@H](CCC%13)C(N[C@H](C(N[C@H](C(N%14[C@@H](CCC%14)C(N)=O)=O)[C@H](CC)C)=O)CC%15=CC=C(O)C=C%15)=O)=O)C)=O)CC(C)C)=O)C)=O)=O)CCCNC(N)=N)=O)CC%16=CNC%17=C%16C=CC=C%17)=O)C(C)C)=O)CCCNC(N)=N)=O)CCCNC(N)=N)=O)C(C)C)=O)CC%18=CN=CN%18)=O)NC%12=O)=O)CCCNC(N)=N)=O)=O)CC%19=CNC%20=C%19C=CC=C%20)=O)CCCNC(N)=N)[C@@H](NC(C)=O)CCCNC(N)=N |
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 | Soluble to 1 mg/ml in water |
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
If you know of a relevant reference for xStAx-VHLL, please let us know.
Keywords: xStAx-VHLL, xStAx-VHLL supplier, β, beta, B, catenin, wnt, signaling, active, degraders, degrades, targeted, protein, degradation, TPD, PROTAC, PROTACs, selective, Beta-catenin, Other, Degraders, 7298, Tocris Bioscience
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:
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