Zincov
Zincov is an orally active hydroxamic acid derivative and bacterial metalloproteinase inhibitor. Zincov blocks chloride ion binding by binding to the active site of thermolysin, thereby inhibiting the hydrolysis and blood coagulation reactions catalyzed by this enzyme. Meanwhile, Zincov attenuates cytotoxicity, prevents protein degradation and ZO-1 rearrangement without affecting the functions of other common proteases. Zincov exhibits blood glucose-regulating and antioxidant activities; it reduces blood glucose levels and increases liver dry weight in diabetic rats, but elevates blood glucose levels in normal rats. Zincov is widely used in studies related to cholera and diabetes.
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- CAS No.: 71431-46-4
- 화학식: C12H22N4O5
- 분자량:302.33
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보관:
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
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
In Vitro
Zincov (0-800 nM; 1 h) inhibits thermolysin-catalyzed FAGLA hydrolysis with a Ki of 180 nM at pH 7.5 and 25°C[1].
Zincov (500 μM; 30 min-3.5 h) potently attenuates HA/P-mediated degradation of occludin in MDCK-I cells[3].
Zincov (500 μM; 15 min) prevents HA/P-mediated rearrangement of ZO-1 in MDCK-I cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Mardin-Darby canine kidney epithelial cell line I (MDCK-I) cells
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Concentration:500 μM
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Incubation Time:30 min; 1 h; 2 h; 3.5 h
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Result:Greatly attenuated the HA/P-mediated degradation of occludin (66-85 kDa) into 50 kDa and 35 kDa fragments, as shown by preservation of the full-length occludin bands and reduction in the intensity of the degradation product bands.
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Cell Line:Mardin-Darby canine kidney epithelial cell line I (MDCK-I) cells
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Concentration:500 μM
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Incubation Time:15 min
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Result:Prevented the HA/P-mediated rearrangement of ZO-1, maintaining ZO-1 as narrow continuous ribbons along cell-cell boundaries, similar to untreated cells.
Chemical Information
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CAS No. 71431-46-4
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분자량 302.33
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화학식 C12H22N4O5
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SMILES
NC(CNC([C@H](C)NC(C(CC(C)C)C(NO)=O)=O)=O)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[1]. Inouye K, et al. A spectrophotometric study on the interaction of thermolysin with chloride and bromide ions, and the state of tryptophyl residue 115. J Biochem. 1994;116(3):530-535. [Content Brief]
[2]. Booth BA, et al. Vibrio cholerae soluble hemagglutinin/protease is a metalloenzyme. Infect Immun. 1983;42(2):639-644. [Content Brief]
[3]. Wu Z, et al. Distinct effects of Vibrio cholerae haemagglutinin/protease on the structure and localization of the tight junction-associated proteins occludin and ZO-1. Cell Microbiol. 2000;2(1):11-17. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Zincov Related Classifications
HY-183878 Related Classifications
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