2. Stem Cell/Wnt Cell Cycle/DNA Damage
  3. β-catenin Wnt CDK
  4. β-catenin-IN-3

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.

β-catenin-IN-3

β-catenin-IN-3 Chemical Structure

CAS No. : 1005288-15-2

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Solution
10 mM * 1 mL in DMSO In-stock
Solid
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Based on 1 publication(s) in Google Scholar

β-catenin-IN-3 Related Antibodies

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1 Publications Citing Use of MCE β-catenin-IN-3

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Description

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[1].

IC50 & Target[1]

Cdk4/cyclin D1

 

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.

β-catenin-IN-3 Related Antibodies

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.
Molecular Weight

484.25

Formula

C19H20Br2N2OS
CAS No.
Appearance

Solid

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)

Purity & Documentation
References
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β-catenin-IN-3 Related Classifications

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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.

Keywords:

β-catenin-IN-31005288-15-2β-cateninWntCDKBeta cateninCyclin dependent kinaseAnticancerWnt pathwayβ-catenin-driven cancer cellstherapeutic targetingInhibitorinhibitorinhibit

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