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KI2517GI254023X1 mg$377

Chemical Characteristic

Product NameGI254023X
SynonymsN/A
CAS No.260264-93-5
Molecular Weight 391.5
FormulaC21H33N3O4
Chemical Name(2R)-N-[(1S)-2,2-Dimethyl-1-[(methylamino)carbonyl]propyl]-2-[(1S)-1-(N-hydroxyformamido)ethyl]-5-phenylpentanamide
SmilesC(=O)([C@H](CCCc1ccccc1)[C@H](C)N(O)C=O)NC(C(C)(C)C)C(=O)NC
Chemical Structure

Biological activities

GI254023X is selective inhibitor of A-Disintegrin and Metalloprotease 10 (ADAM10). GI254023X inhibits ADAM10 and ADAM17 with IC50s of 5.3 and 541 μM, respectively.[1] GI254023X reduces E-cadherin shedding in a dose-dependent manner in HaCaT keratinocytes. GI254023X treatment abolishes the increased release of soluble E-cadherin but also the increase in CTF1 generation. GI254023X rescues E-cadherin cell surface expression and β-catenin translocation after ionomycin treatment.[2]

References

[1] Hoettecke N, et al. Improved synthesis of ADAM10 inhibitor GI254023X. Neurodegener Dis. 2010, 7(4): 232-238.
[2] Maretzky T, et al. ADAM10 mediates E-cadherin shedding and regulates epithelial cell-cell adhesion, migration, and beta-catenin translocation. Proc Natl Acad Sci U S A. 2005, 102(26): 9182-9187.

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