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 (18)
| Target | HGNC Symbol | Additional Synonyms | Data |
|---|---|---|---|
| DUSP22/MKPX | DUSP22 | Dual specificity protein phosphatase 22, JNK-stimulatory phosphatase-1, Low molecular weight dual specificity phosphatase 2, Mitogen-activated protein kinase phosphatase x, JSP1, LMWDSP2 | Data sheet |
| PP1A | PPP1CA | Serine/threonine-protein phosphatase PP1-alpha catalytic subunit, PPP1A | Data sheet |
| PP1B | PPP1CB | Serine/threonine-protein phosphatase PP1-beta catalytic subunit | Data sheet |
| PP2A alpha/PPP2R1A Complex | PPP2CA/PPP2R1A Complex | PP2A alpha: Serine/threonine-protein phosphatase 2A catalytic subunit alpha isoform; PPP2R1A: Serine/threonine-protein phosphatase 2A 65 kDa regulatory subunit A alpha isoform | Data sheet |
| PPAC (ACP1/LMW-PTP-A) | PPAC (ACP1/LMW-PTP-A) | Low molecular weight phosphotyrosine protein phosphatase, Adipocyte acid phosphatase, Low molecular weight cytosolic acid phosphatase, Red cell acid phosphatase 1, LMPTP-A, HCPTP-A | Data sheet |
| PPAC (ACP1/LMW-PTP-B)* | PPAC (ACP1/LMW-PTP-B) | Low molecular weight phosphotyrosine protein phosphatase, Adipocyte acid phosphatase, Low molecular weight cytosolic acid phosphatase, Red cell acid phosphatase 1, LMPTP-B, HCPTP-B | Data sheet |
| PTPN1/PTP1B-CD | PTPN1 | Tyrosine-protein phosphatase non-receptor type 1, Protein-tyrosine phosphatase 1B | Data sheet |
| PTPN1/PTP1B-FL* | PTPN1 | Tyrosine-protein phosphatase non-receptor type 1, Protein-tyrosine phosphatase 1B | Data sheet |
| PTPN11/SHP2 (E76K)-FL | PTPN11 (E76K) | Tyrosine-protein phosphatase non-receptor type 11, Protein-tyrosine phosphatase 1D, Protein-tyrosine phosphatase 2C, SH-PTP2, SH-PTP3, PTP2C, SHPTP2 | Data sheet |
| PTPN11/SHP2-CD | PTPN11 | Tyrosine-protein phosphatase non-receptor type 11, Protein-tyrosine phosphatase 1D, Protein-tyrosine phosphatase 2C, SH-PTP2, SH-PTP3, PTP2C, SHPTP2 | Data sheet |
| PTPN11/SHP2-FL | PTPN11 | Tyrosine-protein phosphatase non-receptor type 11, Protein-tyrosine phosphatase 1D, Protein-tyrosine phosphatase 2C, SH-PTP2, SH-PTP3, PTP2C, SHPTP2 | Data sheet |
| PTPN12/PTP-PEST | PTPN12 | Tyrosine-protein phosphatase non-receptor type 12, Protein-tyrosine phosphatase G1, PTN12 | Data sheet |
| PTPN2/TC-PTP | PTPN2 | Tyrosine-protein phosphatase non-receptor type 2, T-cell protein-tyrosine phosphatase, PTN2, PTPT | Data sheet |
| PTPN6/SHP1 | PTPN6 | Tyrosine-protein phosphatase non-receptor type 6, Hematopoietic cell protein-tyrosine phosphatase Protein-tyrosine phosphatase 1C, Protein-tyrosine phosphatase SHP-1, HCP, PTP1C | Data sheet |
| PTPN7/LC-PTP | PTPN7 | Tyrosine-protein phosphatase non-receptor type 7, Hematopoietic protein-tyrosine phosphatase, PTN7 | Data sheet |
| PTPRB | PTPRB | Receptor-type tyrosine-protein phosphatase beta, Protein-tyrosine phosphatase beta, Vascular endothelial protein tyrosine phosphatase, VE-PTP | Data sheet |
| PTPRC/CD45 | PTPRC | Receptor-type tyrosine-protein phosphatase C, Leukocyte common antigen, T200 | Data sheet |
| PTPRJ/CD148 | PTPRJ | Receptor-type tyrosine-protein phosphatase eta, Protein-tyrosine phosphatase eta, Protein-tyrosine phosphatase receptor type J, Density-enhanced phosphatase 1, DEP1 | Data sheet |
*Phosphatase targets not part of the full screening panels
Phosphatase Assay Details
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.
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.
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