Phosphatase Assays
Target-specific Assays

Phosphatase Assay Services for Drug Discovery

Reaction Biology offers phosphatase assays for compound screening and profiling for drug discovery. Our phosphatase assays are based on the dephosphorylation of the fluorinated MUP (methylumbelliferyl phosphate) derivative which serves as a substrate for most protein phosphatases. Dephosphorylation of MUP generates the fluorescent DiFMUP (6,8-difluoro-4-methylumbelliferyl phosphate) which is quantified for the determination of phosphatase activity.

Protein phosphatases play important roles in cell signaling processes in tandem with kinases. Different than kinases, phosphatases were long considered undruggable because their active site is highly conserved resulting in selectivity issues and an unfavorable molecular composition leading to bioavailability issues. The discovery of an allosteric SHP2 inhibitor paved the road for the creation of further allosteric inhibitors of phosphatases. Our activity assays are an essential tool for phosphatase profiling for allosteric inhibitor discovery.

  • Fluorescence-based phosphatase activity assays
  • High-throughput compatible phosphatase screening
  • Custom-tailored phosphatase screening assay development is possible
  • Deliverable: % inhibition (single point) or IC50 value determination

At Reaction Biology, we offer phosphatase profiling and screening services for pharma, biotech, and academic institutions with a commitment to quality data and quality service. Our global business development team is available to discuss your phosphatase screening needs with you today.

List of Phosphatase Assays (21)

*Phosphatase targets not part of the full screening panels

Phosphatase Assay Details

  • Assay Format
  • Assay Setup
Assay Format

Phosphatase Assay Format

The fluorinated MUP derivative is used as a substrate for a large range of protein phosphatase assays. The reaction product of DiFMUP is fluorescent after dephosphorylation.

Assay Setup

Phosphatase Assay Setup

Setups: Single-dose screening in duplicates or IC50 value determination with 5 or 10 concentrations. Other screening formats are available upon request.

Controls: No inhibitor (DMSO vehicle) control and for every assay, one target-specific control compound is tested in 10-dose IC50 format.

Turnaround time: 10 business days for standard projects. Expedited scheduling and data delivery can be arranged prior to the commencement of the studies.

Report: The raw data, % enzyme activity and control compound IC50 values will be reported in Excel format for single-dose assays. For IC50 orders, raw data, IC50 values, and curve fitting will be delivered in Excel format. Assay conditions, target, and substrate information are available upon request. Requirements for this information should be noted prior to the commencement of the study.

Screening facility: This assay is performed at our screening facility in Malvern, PA, US.

Compound requirements: In brief, for a standard project, 20 µl of a 10 mM DMSO stock or solid material is needed. Less material is needed for large scale screening. Please refer to our FAQs for information regarding compound preparation and shipping.