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Inhibitor Screening

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Inhibition Assays

We are able to offer inhibition assays for any of our products. we can assist with hit identification, determination of IC50 values or investigation into the mechanism of action.

Any number or combination of assays can be carried out and there is no minimum number of compounds required.

All assays are performed in-house by experienced researchers. Results are provided as a full written report containing original gel images or raw data, processed data and subsequent statistical analysis. We have many years of experience working with these types of assays and can quickly identify positive inhibitors saving you time and money. The data ownership is yours and will never be shared; confidentiality is paramount.

Just send us your compounds and we will do the rest.

Topoisomerase Assays

We offer a number of topoisomerase assays which can identify inhibitors, determine IC50 values or investigate the mechanism of action. They include a medium/high-throughput plate-based assay, gel-based supercoiling, relaxation and decatenation reactions, ATPase assays, cleavage assays and DNA unwinding assays.

ATPase Assays

Hydrolysis of ATP is essential for the activity of topoisomerase II enzymes as well as many other DNA modifying enzymes and inhibition of the ATPase activity is the mechanism by which compounds such as coumarins (e.g. novobiocin) inhibit the enzymes. With DNA topoisomerases the activity of the complete enzyme is stimulated by binding DNA (the E.coli GyrB43 domain is not stimulated). The reaction can be followed by a number of methods. In the linked assay, the hydrolysis of ATP is linked to the conversion of NADH to NAD+ which can then be measured by a change in absorbance at 340nm. This is a continuous assay which allows the course of the reaction to be monitored. Details of the assays can be found here. An alternative assay which uses Malachite Green to directly measure the phosphate produced by the hydrolysis of ATP to ADP is an end-point assay. We are also able to supply this assay if you prefer. Please enquire for more information.

Pricing

We offer competitive pricing and can offer discounts for larger projects. Please contact us to discuss your requirements.

Please contact us for a Quote

 

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