β-catenin-IN-10

Cat. No.: HY-P11660: Data Sheet Handling Instructions
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β-catenin-IN-10 is a β-catenin:TCF4 interaction inhibitor with an IC₅₀ of 5.44 μM. β-catenin-IN-10 inhibits the Wnt and AR signaling pathways with IC₅₀ values of 0.105 μM and 1.02 μM, respectively. β-catenin-IN-10 suppresses the proliferation of castration-resistant prostate cancer cells. β-catenin-IN-10 is applicable to research related to prostate cancer.

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

β-catenin-IN-10 Chemical Structure

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Wnt1 Wnt3 Wnt5 Wnt7

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Description

In Vitro

β-catenin-IN-10 (10 μM; 24 h) regulates the expression of Wnt and AR target genes in LNCaP-abl and LNCaP-95 prostate cancer cells, reduces oncogenic target transcripts, and upregulates E-cadherin^[1].
β-catenin-IN-10 (0.195-0.782 μM; 5 d) potently inhibits the proliferation of castration-resistant prostate cancer cells LNCaP-abl and LNCaP-95 in 2D culture systems, with IC₅₀ values of 0.195 μM and 0.782 μM for the two cell lines, respectively, but exerts no effect on non-prostate cancer cells independent of Wnt signaling^[1].
β-catenin-IN-10 (0.694-1.34 μM; 17-22 d) inhibits the proliferation of LNCaP-abl prostate cancer spheroids in a 3D culture system; when the compound is added at the time of seeding, its IC₅₀ is 0.694 μM, whereas when added to pre-formed spheroids, the IC₅₀ is 1.34 μM^[1].

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

Real Time qPCR^[1]

Cell Line:	LNCaP-abl and LNCaP-95 castration-resistant prostate cancer cells
Concentration:	10 μM
Incubation Time:	24 h
Result:	Decreased mRNA levels of Wnt target genes (AR, cMYC, Cyclin D1), AR target genes (PSA, FKBP5), and the constitutively active AR splice variant AR-V7; increased mRNA levels of E-cadherin, a gene repressed by Wnt signaling.

Cell Viability Assay^[1]

Cell Line:	LNCaP-abl, LNCaP-95, U2OS, and A549 cells
Concentration:	0.195 μM IC₅₀ (LNCaP-abl); 0.782 μM IC₅₀ (LNCaP-95); 0.001 to 100 μM (dose range)
Incubation Time:	5 days
Result:	Inhibited proliferation of LNCaP-abl cells with an IC₅₀ of 0.195 μM and LNCaP-95 cells with an IC₅₀ of 0.782 μM; had no effect on proliferation of Wnt-independent U2OS (osteosarcoma) and A549 (lung adenocarcinoma) cells.

Cell Viability Assay^[1]

Cell Line:	LNCaP-abl prostate cancer cells
Concentration:	0.694 μM IC₅₀ (Day 0 addition); 1.34 μM IC₅₀ (Day 5 addition); 0.001 to 100 μM (dose range); ≥1 μM (spheroid formation inhibition/growth stall)
Incubation Time:	22 days total (Day 0 addition, media changes every 3-4 days); 17 days total (Day 5 addition, media changes every 3-4 days)
Result:	When added on Day 0, inhibited spheroid proliferation with an IC₅₀ of 0.694 μM; when added to pre-formed spheroids on Day 5, inhibited proliferation with an IC₅₀ of 1.34 μM. Concentrations ≥1 μM prevented spheroid formation or stalled growth of pre-formed spheroids.

In Vivo

β-catenin-IN-10 (Compound 13) (10 μM; single administration) potently inhibits the hyperactivated Wnt signaling pathway in zebrafish embryos, leading to complete recovery of ocular development in 100% of the treated embryos^[1].

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

Animal Model:	wild-type (embryos)^[1]
Dosage:	10 μM
Administration:	immersion; single dose at 5.5 hours post-fertilization
Result:	Rescued eye development in 100% of embryos (8/8 embryos in each of 3 independent experiments).

Molecular Weight

1412.63

Formula

C₇₄H₉₇N₁₁O₁₇

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Schneider JA, et al. Design of Peptoid-peptide Macrocycles to Inhibit the β-catenin TCF Interaction in Prostate Cancer. Nat Commun. 2018;9(1):4396. Published 2018 Oct 23. [Content Brief]

β-catenin-IN-10 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-10β-cateninWntAndrogen ReceptorBeta catenincastration-resistant prostate cancer cellszebrafishTCF4canonical Wnt signalingWnt signaling pathwayLNCaP-abl cellsLNCaP-95 cellsHEK293 cellsandrogen receptor signaling pathwayInhibitorinhibitorinhibit

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