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.
For research use only. We do not sell to patients.
- CAS No.: 346660-34-2
- Formula: C16H11N5O5S
- Molecular Weight:385.35
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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.
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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CAS No. 346660-34-2
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Molecular Weight 385.35
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Hakin-1 Related Classifications
HY-176861 Related Classifications
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