LZZ-02
LZZ-02 is an orally active Tankyrase 1/2 inhibitor. LZZ-02 reduces c-Myc levels and inhibits the transcriptional activity of the WNT/β-catenin pathway. LZZ-02 exhibits anticancer activity against colon cancer. LZZ-02 can be used in studies related to colorectal cancer.
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- CAS No.: 37418-69-2
- Formule: C15H12N2O3
- Masse moléculaire:268.27
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
LZZ-02 (0.1-100 μM; 24 h) potently inhibits LiCl (HY-Y0649)-induced β-catenin transcriptional activity in HEK293 cells, with an IC50 of 10 μM[2].
LZZ-02 (100 μM; 24 h) potently inhibits Wnt3a-induced β-catenin transcriptional activity in HEK293 cells[2].
LZZ-02 inhibits β-catenin transcriptional activity induced by β-catenin overexpression in HEK293 cells[2].
LZZ-02 (1-100 μM; 24 h) dose-dependently decreases the protein levels of β-catenin, c-Myc and Cyclin D1, while upregulates the protein level of Axin2, in DLD1 colorectal cancer cells[2].
LZZ-02 (30 μM) upregulates the protein level of Axin2 and reduces the protein level of β-catenin in SW480 colorectal cancer cells[2].
LZZ-02 (30 μM; days 1-9) inhibits the proliferation of DLD1 and SW480 colorectal cancer cells, with an effect comparable to that of XAV939[2].
LZZ-02 (30 μM; 2 weeks) inhibits colony formation of DLD1 and SW480 colorectal cancer cells[2].
LZZ-02 inhibits the proliferation of colorectal cancer cell line DLD-1 in vitro[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:DLD1 colorectal cancer cells
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Concentration:1-100 μM (β-catenin, c-Myc, Cyclin D1 analysis); 30 μM (Axin2 analysis)
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Incubation Time:24 h
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Result:Reduced the protein levels of β-catenin, c-Myc, and Cyclin D1 in a dose-dependent manner, with noticeable decreases starting at 25 μM.
Significantly increased Axin2 protein levels while strongly decreasing β-catenin levels at 30 μM.
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Cell Line:DLD1 and SW480 colorectal cancer cells
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Concentration:30 μM
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Incubation Time:1-9 days
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Result:Significantly reduced cell viability in both DLD1 and SW480 cells over the 9-day period, with viability reduced by approximately 20% compared to untreated controls by day 9.
Showed inhibition efficiency comparable to the reference compound XAV939.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (6-week-old female; subcutaneous xenograft model induced by implantation of 2.5 × 106 DLD1 cells)[2]
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Dosage:30 mg/kg
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Administration:p.o.; daily; 18 days
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Result:Reduced average tumor weight to 0.26 g at day 18 post-treatment, compared to 1 g in the control group.
Caused no significant change in mouse body weight during the treatment period.
Chemical Information
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CAS No. 37418-69-2
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Masse moléculaire 268.27
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Formule C15H12N2O3
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SMILES
O=C(C1=CC=CC=C1)/C=C/NC2=CC=C(C=C2)[N+]([O-])=O
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Synonyms
ZINC13406363
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Pećina-Šlaus N, et al. Wnt Signaling Inhibitors and Their Promising Role in Tumor Treatment. International journal of molecular sciences. 2023 Apr 04;24(7):6733. [Content Brief]
[2]. Li B, et al. Discovery of Novel Inhibitor for WNT/β-Catenin Pathway by Tankyrase 1/2 Structure-Based Virtual Screening. Molecules (Basel, Switzerland). 2020 Apr 06;25(7):1680. [Content Brief]
[3]. Yu M, et al. Small-Molecule Inhibitors of Tankyrases as Prospective Therapeutics for Cancer. Journal of medicinal chemistry. 2022 Apr 14;65(7):5244-5273. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LZZ-02 Related Classifications
HY-183474 Related Classifications
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