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AM 114

In stock
Catalog No.
A8163
20S proteasome inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$50.00
In stock
Evaluation Sample
$28.00
In stock
10mg
$60.00
In stock
25mg
$120.00
In stock
50mg
$200.00
In stock

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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

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.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at 4°C
M.Wt377.01
Cas No.856849-35-9
FormulaC20H21B2NO5
Solubility≥16.65mg/mL in DMSO
Chemical Name[4-[(Z)-[(5Z)-5-[(4-boronophenyl)methylidene]-1-methyl-4-oxopiperidin-3-ylidene]methyl]phenyl]boronic acid
SDFDownload SDF
Canonical SMILESB(C1=CC=C(C=C1)C=C2CN(CC(=CC3=CC=C(C=C3)B(O)O)C2=O)C)(O)O
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor 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.

Biological Activity

Targets Proteasome          
IC50 1 μM          

Quality Control

Chemical structure

AM 114

Related Biological Data

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Related Biological Data

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Related Biological Data

AM 114