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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- No. CAS: 346660-34-2
- Fòrmula: C16H11N5O5S
- Peso molecular:385.35
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Almacenamiento:
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Actividad biológica
Descripciòn
In Vitro
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.
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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.
In Vivo
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.
Chemical Information
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No. CAS 346660-34-2
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Peso molecular 385.35
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Hakin-1 Related Classifications
HY-176861 Related Classifications
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