Cat. No.: HY-147007

β-catenin-IN-3

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

β-catenin-IN-3 (Compound C2) is a selective β-catenin inhibitor. β-catenin-IN-3 binds to allosteric site on the surface of β-catenin with K_D calculated at 54.96 nM. β-catenin-IN-3 selectively inhibits β-catenin via targeting a cryptic allosteric modulation site, lowers its cellular load. β-catenin-IN-3 significantly reduces viability of β-catenin driven cancer cells, and triggers β-catenin degradation via proteasome system in β-catenin-overexpressing cancer cells.

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

Purity: 95.64%
CAS No.: 1005288-15-2
Formula: C₁₉H₂₀Br₂N₂OS
Molecular Weight:484.25

Storage:

-20°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

β-catenin-IN-3 Chemical Structure

CAS No.: 1005288-15-2

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

Cdk4/cyclin D1

All Wnt Isoforms :

All CDK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
SW480	IC₅₀	1.35 μM Compound: 65; C2	Antiproliferative activity against human SW480 cells assessed as inhibition of cell growth incubated for 72 hrs by alamar blue assay Antiproliferative activity against human SW480 cells assessed as inhibition of cell growth incubated for 72 hrs by alamar blue assay	[PMID: 36183504]

In Vitro

β-catenin-IN-3 (24 h) reduces viability of DLD1, SW480, HCT116,SW48, MCF10A and H460 cells in dose-dependent manner with IC₅₀s of 0.85 μM, 1.35 μM, 5.35 μM, 3.45 μM, and above 20μM^[1].
β-catenin-IN-3 (1, 3 μM, 7 days) inhibits the colony forming ability of DLD1 and SW48 cells^[1].
β-catenin-IN-3 (0, 1, 5μM, 24 h) selectively inhibits levels of β-catenin, Axin1, CyclinD1 and TCF4 in dose-dependent manner in DLD1 and SW480 cells ^[1].
β-catenin-IN-3 (1 μM, 3 h) triggers degradation of β-catenin in DLD1 cells through ubiquitin-proteasome machinery, presumably via recruitment of the APC-mediated destruction complex ^[1].
β-catenin-IN-3 (1 μM, 1-24 h) increases phosphorylation of β-catenin in DLD1 cells ^[1].
β-catenin-IN-3 (1, 5 μM, 24 h) reduces β-cateninin in the nuclear and cytoplasmic fractions to 45%, 40%, 85% and 55%, respectively^[1].
β-catenin-IN-3 (3, 5μM, 4 days) inhibits APC-deficient organoid clonogenicity viability around 70% and 55%, on the contrary, viability of wild-type organoids is 90%. ^[1].

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

Cell Viability Assay^[1]

Cell Line:

DLD1,SW4808, HCT116, SW48, MCF10A, H460 cells
Concentration:

10 nM-100 μM
Incubation Time:

24 h
Result:

Reduced viability of DLD1 and SW480 cells in dose-dependent manner with IC₅₀s of 0.85 μM and 1.35 μM.
Reduced viability of HCT116 and SW48 cells in dose-dependent manner with IC₅₀s of 5.35 μM and 3.45 μM.
Impacted two WNT-independent cell lines, MCF10A and H460, with IC₅₀ above 20μM.

Western Blot Analysis^[1]

Cell Line:

DLD1 cells
Concentration:

1μM
Incubation Time:

1,3,6,12,24 h
Result:

Phosphorylated β-catenin starting at 1 hour point, which was further amplified to 2-2.5-fold at 12 and 24 hour points, and can be blocked by CHIR99021 (HY-10182).
Levels of active β-catenin markedly reduced at these time points, and can be arrested by MG132 (HY-13259).

Immunofluorescence^[1]

Cell Line:

DLD1 cells
Concentration:

1 μM
Incubation Time:

24 h
Result:

Reduced β-catenin that co-localized with nucleic acids inside the nucleus by 55-60% (co-localization dropped from 0.62 to 0.25).

In Vivo

β-catenin-IN-3 (25 mg/kg, i.p., 35 days) notably reduces β-catenin-dependent tumor growth represented in DLD1 xenograft model^[1].

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

Animal Model:

6-week-old female NSG (NOD-SCID) mice were injected with 3 *10⁶ DLD1 cells^[1].
Dosage:

25 mg/kg
Administration:

i.p., 35 days
Result:

Mice Did not display any signs of acute toxicity and body weight loss.
Inhibition of tumor growth by β-catenin-IN-3 was noted after 20 days of treatment, after which the tumor volume of β-catenin-IN-3 treated mice did not increase exponentially.
At day 35, the calculated tumor growth inhibition by β-catenin-IN-3 was 50% as compared to the vehicle.

Chemical Information

CAS No. 1005288-15-2
Appearance Solid
Molecular Weight 484.25
Formula C₁₉H₂₀Br₂N₂OS
Color White to off-white
SMILES

S=C(N/C=C/C(C=C1Br)=C(C(Br)=C1)O)NC(C2)C3C(C=CC4)C4C2C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Publications (1)

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Journal Impact Factor

J Pharm Pharmacol

Aucubin inhibits the activity of lung cancer stem-like cells by targeting degradation of β-catenin. [Abstract]

2025 Sep 10:rgaf081. PMID: 40928458

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (206.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0650 mL

10.3252 mL

20.6505 mL

5 mM

0.4130 mL

2.0650 mL

4.1301 mL

10 mM

0.2065 mL

1.0325 mL

2.0650 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight Molecular Weight

Dilution Calculator

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.16 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.16 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.16 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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g
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Cheltsov A, et al. Allosteric inhibitor of β-catenin selectively targets oncogenic Wnt signaling in colon cancer. Sci Rep. 2020;10(1):8096. Published 2020 May 15. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0650 mL	10.3252 mL	20.6505 mL	51.6262 mL
	5 mM	0.4130 mL	2.0650 mL	4.1301 mL	10.3252 mL
	10 mM	0.2065 mL	1.0325 mL	2.0650 mL	5.1626 mL
	15 mM	0.1377 mL	0.6883 mL	1.3767 mL	3.4417 mL
	20 mM	0.1033 mL	0.5163 mL	1.0325 mL	2.5813 mL
	25 mM	0.0826 mL	0.4130 mL	0.8260 mL	2.0650 mL
	30 mM	0.0688 mL	0.3442 mL	0.6883 mL	1.7209 mL
	40 mM	0.0516 mL	0.2581 mL	0.5163 mL	1.2907 mL
	50 mM	0.0413 mL	0.2065 mL	0.4130 mL	1.0325 mL
	60 mM	0.0344 mL	0.1721 mL	0.3442 mL	0.8604 mL
	80 mM	0.0258 mL	0.1291 mL	0.2581 mL	0.6453 mL
	100 mM	0.0207 mL	0.1033 mL	0.2065 mL	0.5163 mL

Keywords

β-catenin-IN-3

1 Cited Publications

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β-catenin-IN-3

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Stem Cell Signaling Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

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Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Transcription Factor-Targeted Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Antihypertensive Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Extracellular Vesicles (EVs) Compound Library

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Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

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Anti-Brain Cancer Compound Library

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High-Throughput Bioactive Compound Library

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Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Publications Citing Use of MedChemExpress (MCE) β-catenin-IN-3

All Wnt Isoforms

All CDK Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

β-catenin-IN-3 Related Classifications

Cat. No.: HY-147007