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
- Protocols
- 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. Further protocols information, click here.
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.
Protocols
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Cell migration
Cell migration is a method that plays an important role in wound healing, cell differentiation, embryonic development, etc.
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
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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