Wnt/β-catenin-IN-6 

Wnt/β-catenin-IN-6 is an orally active Wnt/β-catenin pathway inhibitor. Wnt/β-catenin-IN-6 blocks the AKT/GSK-3β/β-catenin signaling pathway, leading to reduced expression of Wnt target genes (c-Myc, c-Jun). Wnt/β-catenin-IN-6 reduces COX2 expression and IL-8 levels, highlighting its dual anti-inflammatory and antitumor effects. Wnt/β-catenin-IN-6 can induce apoptosis. Wnt/β-catenin-IN-6 serves as a tool for non-small cell lung cancer (NSCLC) research^[1].

Wnt/β-catenin-IN-6 (Compound B10) (72 h), demonstrates potent cytotoxic activity toward human non-small cell lung cancer cell line A549 (IC₅₀ = 1.28 μM), with IC₅₀ values of 3.74, 3.22, 5.68 μM in SKOV3, MDAMB-231, BEAS-2B cells respectively^[1].
Wnt/β-catenin-IN-6 (2, 4 μM, 48 h) shows potent antiproliferative effect by suppressing the EGFR/Erk signaling pathway in A549 cells^[1].
Wnt/β-catenin-IN-6 (4 μM, 72 h) induces only 10 % apoptotic response, with no significant difference from the control group in A549 cells^[1].
Wnt/β-catenin-IN-6 (2, 4 μM, 48 h) inhibits the Wnt/β-catenin signaling pathway in A549 cells via the AKT/GSK-3β/β-catenin axis^[1].
Wnt/β-catenin-IN-6 (2, 4 μM, 48 h) downregulates the IL-8 mRNA expression in A549 cells as well as the expression of c-Myc and c-Jun, suggesting the inflammation-suppression effect^[1].

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

Wnt/β-catenin-IN-6 (compound B10) (25 mg/kg, i.g., every other day) possesses significant anti-NSCLC activity and favorable biosafety in an A549 xenograft model established in male BALB/C nude mice^[1].
Wnt/β-catenin-IN-6 (12.5-50 mg/kg, i.g., once) exhibits no observable toxicity in ICR mice at doses up to 50 mg/kg^[1].

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

426.47

C₂₅H₂₂N₄O₃

Solid

Light yellow to yellow

COC1=C(OCC2=CC=CC=C2)C=C(N=CN=C3NC4=CC=C(NC(C=C)=O)C=C4)C3=C1

Room temperature in continental US; may vary elsewhere.

* 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Zhao M, et al. A novel Quinazoline derivative exerts anti-tumor effects in non-small cell lung cancer through Wnt/β-catenin pathway inhibition. Bioorg Chem. 2025 Jun 15;160:108481.  [Content Brief]