Home>>Signaling Pathways>> Ubiquitination/ Proteasome>> Proteasome>>AM 114
AM 114 Catalog No.GC13789

20S proteasome inhibitor

Size Price Stock Qty
10mg
$195.00
In stock
50mg
$792.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical Properties

Cas No. 856849-35-9 SDF
Synonyms N/A
Chemical Name [4-[(Z)-[(5Z)-5-[(4-boronophenyl)methylidene]-1-methyl-4-oxopiperidin-3-ylidene]methyl]phenyl]boronic acid
Canonical SMILES B(C1=CC=C(C=C1)C=C2CN(CC(=CC3=CC=C(C=C3)B(O)O)C2=O)C)(O)O
Formula C20H21B2NO5 M.Wt 377.01
Solubility ≥16.65mg/mL in DMSO, ≥4.11 mg/mL in EtOH with ultrasonic, <2.7 mg/mL in H2O Storage Store at 4°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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Background

AM 114, a derivative of boronic chalcone, is a potent small-molecule inhibitor of the proteasome that inhibits the chymotrypsin-like activity of the 20S proteasome, with a value of 50% inhibition concentration IC50 of approximately 1 μM, resulting in a significant accumulation of ubiquitinated p53 and other cellular proteins in whole cells without significantly disrupting the interaction of p53 and murine double minute 2 (mdm2) proteins. AM 114 also exerts anti-cancer activity against cancer cells, which potently inhibits the growth of human colon cancer HCT116 cells with values of IC50 of 1.5 μM and 0.6 μM in MTT and colony formation assays respectively.

Reference

[1].Achanta G, Modzelewska A, Feng L, Khan SR, Huang P. A boronic-chalcone derivative exhibits potent anticancer activity through inhibition of the proteasome. Mol Pharmacol. 2006 Jul;70(1):426-33. Epub 2006 Apr 24.