Z-VAE(OMe)-FMK
Z-VAE (OMe)-FMK is a selective inhibitor of UCHL1, with better selectivity over UCHL3 and UCHL5. Z-VAE (OMe)-FMK binds to the active site cleft, covalently modifies the active site cysteine C90 to form a thioether bond, binds to inactive UCHL1 with a misaligned catalytic triad, and acts via a two-step addition-folding/migration/displacement mechanism. Z-VAE (OMe)-FMK stabilizes interactions through hydrogen bonding with oxyanion hole residues and van der Waals interactions with surrounding residues. Z-VAE (OMe)-FMK can be used in research related to colorectal cancer, lung cancer, pancreatic cancer, and Alzheimer's disease.
For research use only. We do not sell to patients.
- CAS No.: 1027141-02-1
- Formula: C23H32FN3O7
- Molecular Weight:481.52
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
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UCHL1 |
In Vitro
Z-VAE(OMe)-FMK (100 μM) irreversibly inhibits purified recombinant UCHL1 by covalently modifying active-site Cys90, binds to the enzyme's inactive, misaligned catalytic triad conformation, and does not inhibit purified recombinant UCHL3 or UCHL5 at the same concentration[1].
Z-VAE(OMe)-FMK binds covalently and specifically to the active site of purified UCH-L1 protein via interactions with residues C90, S89, N88, Q84, N159, R178, and M6, as observed in a 2.35 Å resolution co-crystal structure[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1027141-02-1
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Molecular Weight 481.52
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Formula C23H32FN3O7
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SMILES
[C@H](NC([C@@H](NC([C@@H](NC(OCC1=CC=CC=C1)=O)[C@H](C)C)=O)C)=O)(CCC(OC)=O)C(CF)=O
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Sequence
{Cbz}-VA-{NH-CH2(S-CO-CH2F)-C2-COOMe}
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Sequence Shortening
{Cbz}-Val-Ala-{NH-CH2(S-CO-CH2F)-C2-COOMe}
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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)
Z-VAE(OMe)-FMK Related Classifications
HY-P0112 Related Classifications
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