Hakin-1
Hakin-1 is a E3 Ubiquitin-Ligase Hakai inhibitor. Hakin-1 blocks Hakai-mediated global ubiquitination and specific ubiquitination of E-cadherin and inhibits epithelial-mesenchymal transition (EMT) progression. Hakan-1 inhibits tumor progression and cancer metastasis. Hakin-1 can be used for the study of carcinoma such as colorectal cancer.
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- CAS 番号: 346660-34-2
- 分子式: C16H11N5O5S
- 分子量:385.35
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
体外実験
Hakin-1 (10-3000 μM) exhibits dose-dependent inhibitory effects on the viability of HT-29, LoVo, MDCK, HaKai-MDCK (clone-4) and HaKai-MDCK (clone-11) cells with IC50 of 289.2, 159.1, 265.6, 176.3 and 165.4 μM[1].
Hakin-1 (50-100 μM) promotes the upregulation of E-cadherin and Cortactin, and downregulates Vimentin, but there is no change in mRNA levels in HT-29 cells[1].
Hakin-1 (50-100 μM, 21-28 days) significantly reduces the formation of cancer cell colonies in HT-29 and HaKai-MDCK cells[1].
Hakin-1 (50-100 μM, 48 h) reduces cell invasion and cell migration in HT-29, LoVo and HaKai-MDCK cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:HT-29, LoVo and HaKai-MDCK cells
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Concentration:50 and 100 μM
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Incubation Time:24 h
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Result:Strongly inhibited the migratory ability of HT-29 cells.
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Cell Line:HT-29, LoVo and HaKai-MDCK cells
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Concentration:50 and 100 μM
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Incubation Time:24 h
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Result:Strongly inhibited the invasive ability of LoVo cells.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Hakai-MDCK induced xenografts model established in six weeks old athymic nu/nu mice[1]
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Dosage:5 mg/kg
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Administration:Intraperitoneal injection (i.p.), 3 times a week for 20 days
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Result:Inhibited tumor growth and promoted tumor differentiation.
Significantly reduced the number of Ki67-positive cells, which are markers of tumor proliferation, and the mitotic index.
Significantly reduced the density of blood vessels within the tumor (as indicated by CD31 labeling).
Reduced the level of N-cadherin and increased Cortactin.
Significantly reduced pulmonary micrometastases.
No obvious systemic toxicity.
化学情報
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CAS 番号 346660-34-2
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分子量 385.35
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分子式 C16H11N5O5S
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SMILES
O=C(C1=CC=C(N2N=NN=C2SCC(C3=CC=C([N+]([O-])=O)C=C3)=O)C=C1)O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)