MSTI Fluorescence High-Throughput Drug Assay

This novel fluorescence-based high throughput assay allows for the detection of thiol-reactive drug candidates that are likely to irreversibly interact with biological targets. These promiscuous inhibitors can be identified rapidly, in parallel, for small molecule screening libraries using 384 or 1536 well plate formats. Testing small molecules for their ability to modulate cysteine residues of […]

Contributors

Institute
University of Wisconsin-Milwaukee
Cat. #: 153815
Tool sub type: Fluorescent Probe
Research Fields: Drug development
Product description: This novel fluorescence-based high throughput assay allows for the detection of thiol-reactive drug candidates that are likely to irreversibly interact with biological targets. These promiscuous inhibitors can be identified rapidly, in parallel, for small molecule screening libraries using 384 or 1536 well plate formats. Testing small molecules for their ability to modulate cysteine residues of proteins in the early stages of drug discovery is expected to increase efficiency and success of ev…
Additional notes: ▪<b>More accurate</b> – Less interference from molecules due to use of far red spectrum▪ <b>Faster</b> – Can be used for high throughput screening (1536-well plate format)▪ <b>More versatile</b> – Identifies both electrophilic and redox reactive compounds▪ <b>Stable product</b> – Use of acetylated precursor allows for storage of the assay probe and itsreliable generation in situ
Molecular weight: 294.1
Storage conditions: -20° C, protect from light
Solubility: DMSO, DMF, methanol, water (partially)
References:

McCallum et al. 2013. J Biomol Screen. 18(6):705-13. PMID: 23446699.

High-throughput identification of promiscuous inhibitors from screening libraries with the use of a thiol-containing fluorescent probe.

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