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AM 114 20S proteasome inhibitor

Catalog No.A8163
Size Price Stock 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

Tel: +1-832-696-8203

Email: [email protected]

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1.Chen, Wei, et al. "Competitive Expression of Endogenous Wheat CENH3 May Lead to Suppression of Alien ZmCENH3 in Transgenic Wheat× Maize Hybrids." Journal of Genetics and Genomics (2015).
2. Gunderwala A, Porter J. "A luminescence assay for natural product inhibitors of the Mycobacterium tuberculosis proteasome." Phytochem Anal. 2016 Mar;27(2):126-32. PMID:26778282

Quality Control

Chemical structure

AM 114

Related Biological Data

AM 114

Related Biological Data

AM 114

Related Biological Data

AM 114

Biological Activity

Targets Proteasome          
IC50 1 μM          

AM 114 Dilution Calculator

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AM 114 Molarity Calculator

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Chemical Properties

Cas No. 856849-35-9 SDF Download SDF
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 Storage Store at 4°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
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.

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

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.