1. PROTAC Stem Cell/Wnt
  2. PROTACs β-catenin Wnt
  3. xStAx-VHLL TFA

xStAx-VHLL TFA is a β-catenin PROTAC degrader that promotes ubiquitination and proteasome degradation of β-catenin. xStAx-VHLL TFA inhibits the Wnt/β-catenin signaling pathway. xStAx-VHLL TFA can inhibit the proliferation of colon cancer cells and has anti-tumor activity.

For research use only. We do not sell to patients.

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xStAx-VHLL TFA Chemical Structure

xStAx-VHLL TFA Chemical Structure

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Based on 1 publication(s) in Google Scholar

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Description

xStAx-VHLL TFA is a β-catenin PROTAC degrader that promotes ubiquitination and proteasome degradation of β-catenin. xStAx-VHLL TFA inhibits the Wnt/β-catenin signaling pathway. xStAx-VHLL TFA can inhibit the proliferation of colon cancer cells and has anti-tumor activity[1].

In Vitro

Non-salt dose:
xStAx-VHLL (10-60 μM; 1-6 days) induces β-catenin degradation in a dose-dependent manner in colorectal cancer cells and inhibits cell proliferation[1].
xStAx-VHLL (50-90 μM; 24 h) inhibits Wnt/β-catenin signaling in HEK293T cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: HCT116 cells
Concentration: 10, 20, 30, 40, 50 and 60 μM
Incubation Time: 24 h
Result: Reduced the level of β-catenin in a dose-dependent manner.
In Vivo

Non-salt dose:
xStAx-VHLL (30 mg/kg; Intraperitoneal injection; 14 days) has antitumor activity in mouse intestinal tumor model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: APC min/+ mice that harbored a point mutation in the APC gene, resulting in APC deletion and constitutive activation of Wnt signaling (APC min/+ mice develops intestinal tumors around 10 weeks-old) [1]
Dosage: 30 mg/kg
Administration: Intraperitoneal injection (i.p.); 14days
Result: Dramatically reduced tumor number.
Reduced the active of β-catenin protein levels.
Molecular Weight

3231.89 (free base)

Formula

C154H244N48O29.xC2HF3O2

Appearance

Solid

Color

White to off-white

Sequence

Ac-Arg-Arg-Trp-Pro-Arg-{S5}-Ile-Leu-Asp-{S5}-His-Val-Arg-Arg-Val-Trp-Arg-{Ahx}-Ala-Leu-Ala-Pro-Tyr-Ile-Pro-NH2

Sequence Shortening

Ac-RRWPR{S5}ILD{S5}HVRRVWR-{Ahx}-ALAPYIP-NH2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture and light

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (Need ultrasonic)

DMSO : 100 mg/mL (Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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This equation is commonly abbreviated as: C1V1 = C2V2

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Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.22%

References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
xStAx-VHLL TFA
Cat. No.:
HY-P5819A
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