drug discovery OR stratm Search Results

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			96-Well Plate

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	48-602MAG	Buffer Detection Kit for Magnetic Beads	1 Kit

A novel drug discovery strategy: mechanistic investigation of an enantiomeric antitumor agent targeting dual p53 and NF-κB pathways.
The p53 and nuclear factor κB (NF-κB) pathways play crucial roles in human cancer development. Simultaneous targeting of both pathways is an attractive therapeutic strategy against cancer. In this study, we report an antitumor molecule that bears a pyrrolo[3,4-c]pyrazole scaffold and functions as an enantiomeric inhibitor against both the p53-MDM2 interaction and the NF-κB activation. It is a first-in-class enantiomeric inhibitor with dual efficacy for cancer therapy. Synergistic effect was observed in vitro and in vivo. Docking and molecular dynamics simulation studies further provided insights into the nature of stereoselectivity.
Document Type:

Reference

Product Catalog Number:

07-575
Drug Discovery and Development
Document Type:

Brochure
Toxicology in drug discovery and development: Biomarkers and model organisms
Document Type:

Posters

Product Catalog Number:

Multiple
Product Catalog Name:

Multiple
A plate-based assay to measure cellular ERK substrate phosphorylation: utility for drug discovery of the MAPK-signaling cascade.
The Ras, Raf, mitogen-activated protein kinase kinase (MEK) and extracellular signal-regulated kinase (ERK) signaling cascade is critically involved in cellular signaling with activating mutations in Ras and Raf present in many human tumors. Each constituent of this pathway is considered an important target for pharmaceutical intervention. The terminal kinase ERK is known to phosphorylate p90RSK among myriad substrates, yet robust plate-based high-throughput cellular assays monitoring such activity are not commercially available. In this study, we have utilized the Meso Scale Discovery platform to develop a plate-based assay to monitor the level of phosphorylation of p90RSK. This method is highly robust and can be used to evaluate a large number of inhibitors of ERK, MEK, or Raf in a variety of cellular backgrounds. Furthermore, this assay can be used to quantify the level of phospho-p90RSK in tumor lysates to function as a valuable pharmacodynamic readout.
Document Type:

Reference

Product Catalog Number:

04-419
Advances in high content screening for drug discovery.
Document Type:

Reference

Product Catalog Number:

Multiple
Product Catalog Name:

Multiple
Automated Screening of Aqueous Compound Solubility in Drug Discovery
Document Type:

Posters
Automation: Automated applications support for genomics, proteomics and drug discovery
Document Type:

Data Sheet
Poster: Chemotaxis and Angiogenesis Assays in a 96-well Format for Use in High-Throughput Drug Discovery
Document Type:

Posters
Poster: Development of Invasion and Transendothelial Migration Assays in a 96-well Format for Use in High-Throughput Drug Discovery.
Document Type:

Posters
PREDICTION OF SKIN PERMEATION BY CHEMICAL COMPOUNDS USING THE ARTIFICIAL MEMBRANE, STRAT-M™
PURPOSE:
The usefulness of the synthetic membrane, Strat-M™ as an alternative to human and animal skins was evaluated by estimating the skin permeabilities of chemical compounds.
METHOD:
Thirteen chemical compounds with molecular weights (M.W.) of 152-289 and lipophilicities (log Ko/w) of -0.9 to 3.5 were selected. Strat-M™, excised human skin, or hairless rat skin was set in a Franz-type diffusion cell and a saturated solution of each chemical compound was applied to determine membrane permeation profiles. The obtained permeability coefficients (log P) were compared among these membranes.
RESULTS AND DISCUSSION:
Elevations were observed in log P for Strat-M™ with an increase in the log Ko/w of the applied compounds, and similar results were observed with the human and hairless rat skins. A correlation was obtained in log P values between Strat-M™ and human or hairless rat skin. Furthermore, the diffusion and partition parameters of chemicals in Strat-M™ were similar to those in the excised human and rat skins. These results suggest that Strat-M™ could be used as an alternative to animal or human skin in permeation studies.
Document Type:

Reference

Product Catalog Number:

Multiple
Product Catalog Name:

Multiple

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drug discovery OR stratm

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A novel drug discovery strategy: mechanistic investigation of an enantiomeric antitumor agent targeting dual p53 and NF-κB pathways.

Drug Discovery and Development

Toxicology in drug discovery and development: Biomarkers and model organisms

A plate-based assay to measure cellular ERK substrate phosphorylation: utility for drug discovery of the MAPK-signaling cascade.

Advances in high content screening for drug discovery.

Automated Screening of Aqueous Compound Solubility in Drug Discovery

Automation: Automated applications support for genomics, proteomics and drug discovery

Poster: Chemotaxis and Angiogenesis Assays in a 96-well Format for Use in High-Throughput Drug Discovery

Poster: Development of Invasion and Transendothelial Migration Assays in a 96-well Format for Use in High-Throughput Drug Discovery.

PREDICTION OF SKIN PERMEATION BY CHEMICAL COMPOUNDS USING THE ARTIFICIAL MEMBRANE, STRAT-M™

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