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Inhibitor of the chymotrypsin-like activity of the 20S proteasome (IC50 ~ 1 μM). Displays anticancer activity; inhibits cell growth in human colon cancer HCT116 p53+/+ cells (IC50 = 1.49 μM).
Sold with the permission of Johns Hopkins University
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 377.01. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.1 mM||26.52 mL||132.62 mL||265.24 mL|
|0.5 mM||5.3 mL||26.52 mL||53.05 mL|
|1 mM||2.65 mL||13.26 mL||26.52 mL|
|5 mM||0.53 mL||2.65 mL||5.3 mL|
References are publications that support the biological activity of the product.
Achanta et al (2006) A boronic-chalcone derivative exhibits potent anticancer activity through inhibition of the proteasome. Mol.Pharmacol. 70 426 PMID: 16636137
Achanta et al (2005) Preferential killing of cancer cells with wild-type p53 by boronic chalcones. Proc.Am.Assoc.Cancer Res.Abstr. 46 6162
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Keywords: AM 114, AM 114 supplier, 20S, proteasome, inhibitors, inhibits, Proteinases, Proteases, AM114, Proteasome, 2564, Tocris Bioscience
1 Citation for AM 114
Citations are publications that use Tocris products. Selected citations for AM 114 include:
Dasgupta et al (2014) Proteasome inhibitors alter levels of intracellular peptides in HEK293T and SH-SY5Y cells. PLoS One 9 e103604 PMID: 25079948
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Targeted Protein Degradation Research Product Guide
This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:
- Active Degraders (e.g. PROTACs)
- Degrader Building Blocks
- Custom Degrader Services
- UPS Proteins and Assays
- Assays for Protein Degradation
Targeted Protein Degradation Poster
Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed.