2. Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling MAPK/ERK Pathway Immunology/Inflammation PI3K/Akt/mTOR Apoptosis
  3. Wnt β-catenin EGFR ERK COX Akt GSK-3 c-Myc Apoptosis Interleukin Related JNK
  4. 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 serves as a tool for non-small cell lung cancer (NSCLC) research.

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

Wnt/β-catenin-IN-6

Wnt/β-catenin-IN-6 Chemical Structure

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Wnt/β-catenin-IN-6 Related Antibodies

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Description

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 serves as a tool for non-small cell lung cancer (NSCLC) research[1].

IC50 & Target[1]

COX-2

 

EGFR

 

GSK-3β

 

ERK

 

IL-8

 

Akt

 

JNK

 

In Vitro

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 Related Antibodies

Western Blot Analysis[1]

Cell Line: A549 cells
Concentration: 2, 4 μM
Incubation Time: 48 h
Result: Reduced the phosphorylation levels of EGFR and Erk in A549 cells under basal conditions (without exogenous EGF).
Led to a significant decrease in the expression of phosphorylated EGFR in the presence of EGF, while the inhibition of Erk phosphorylation was less pronounced.

Western Blot Analysis[1]

Cell Line: A549 cells
Concentration: 2, 4 μM
Incubation Time: 48 h
Result: Reduced significantly COX2 expression in A549 cells.
Led to a significant reduction in p-AKT levels and the p-AKT to AKT ratio.
Decreased the level of p-GSK-3β dramatically, as well as the ratio of p-GSK-3β to GSK-3β, which in turn led to the downregulation of active (non-phosphorylated) β-catenin.

Real Time qPCR[1]

Cell Line: A549 cells
Concentration: 2, 4 μM
Incubation Time: 48 h
Result: Downregulated the IL-8 mRNA expression in A549 cells, suggesting the inflammation-suppression effect.
Downregulated the expression of c-Myc and c-Jun.
In Vivo

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.

Animal Model: An A549 xenograft model established in male BALB/C nude mice (6 weeks)[1]
Dosage: 25 mg/kg
Administration: intragastric gavage (i.g.) every other day
Result: Induced no significant differences in body weight, suggesting good systemic tolerance.
Induced no apparent pathological abnormalities.
Exhibited attenuated tumor growth, showing notably stronger tumor inhibition than Gefitinib.
Triggered a marked reduction in Ki67 expression, indicating effective suppression of tumor cell proliferation.
Revealed no evident histopathological abnormalities.
Animal Model: ICR mice (20 males and 20 females, 5-6 weeks)[1]
Dosage: 12.5, 25, 50 mg/kg
Administration: intragastric gavage (i.g.)
Result: Induced no significant body weight loss.
Induced no apparent pathological abnormalities.
Molecular Weight

426.47

Formula

C25H22N4O3
SMILES

COC1=C(OCC2=CC=CC=C2)C=C(N=CN=C3NC4=CC=C(NC(C=C)=O)C=C4)C3=C1
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
References
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Wnt/β-catenin-IN-6 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:

Wnt/β-catenin-IN-6Wntβ-cateninEGFRERKCOXAktGSK-3c-MycApoptosisInterleukin RelatedJNKBeta cateninEpidermal growth factor receptorErbB-1HER1Extracellular signal regulated kinasesCyclooxygenasePKBProtein kinase BGlycogen synthase kinase-3Glycogen synthase kinase 3MycILc-Jun N-terminal kinaseNSCLCanti-inflammatoryantitumor agentsAKTGSK-3βCOX2Inhibitorinhibitorinhibit

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