Phosphatases are critical enzymes that regulate a wide range of cellular processes by removing phosphate groups from proteins, lipids, and other molecules. They play a central role in signal transduction, cell cycle regulation, and apoptosis. Aberrations in phosphatase activity are implicated in various diseases, including cancer, diabetes, and neurodegenerative disorders.
Small molecules and biologics designed to modulate phosphatase activity have shown potential in preclinical and clinical settings. Advances in high-throughput screening technologies, along with a deeper understanding of phosphatase structure and function, have accelerated the discovery of selective inhibitors. However, the complex regulation of phosphatases, often involving multiple isoforms and interacting partners, adds the difficulty in identifying effective therapeutics.
Our service utilizes advanced fluorescence intensity techniques to target and measure phosphatase activity with precision. 6,8-Difluoro-4-methylumbelliferyl phosphate (DiFMUP) is a commonly used fluorescent substrate that, upon interaction with a phosphatase, is hydrolyzed from a non-fluorescent DiFMUP into a highly fluorescent umbelliferone. This umbelliferone exhibits excellent spectral characteristics, and changes in the fluorescence signal can be quantitatively measured using a fluorescence plate reader, thereby assessing the activity of the phosphatase.
| Target | Synonyms | Reference Compound | Assay Format |
|---|---|---|---|
| PP1A | PPP1CA | CalyculinA | FI |
| PP1B | PTPN1, PTN1 | CalyculinA | FI |
| PP2A | CalyculinA | FI | |
| λPP | Na3VO4 | FI | |
| PP5 | PPP5C, PPP5 | Na3VO4 | FI |
| PTPN1 | PTN1, PTP1B | AC484 | FI |
| PTPN2 | TCPTP, PTPT | AC484 | FI |
| PTPN4 | MEG-1 | Na3VO4 | FI |
| SHP1 | PTPN6, HCP, PTP1C | PHPS1 | FI |
| PTPN7 | LC-PTP | Na3VO4 | FI |
| PTPN9 | MEG-2 | Na3VO4 | FI |
| SHP2 | PTPN11, PTP2C, SHPTP2 | TNO155 | FI |
| SHP2(D61G) | / | TNO155 | FI |
| SHP2(E76K) | / | Migoprotafib | FI |
| SHP2(T73I) | / | TNO155 | FI |
| SHP2(N308S) | / | TNO155 | FI |
| SHP2(N308D) | / | TNO155 | FI |
| YopH (Bacteria) | yop2b | Na3VO4 | FI |
| PTPN12 | / | Na3VO4 | FI |
| PTPN13 | PNP1, PTP1E, PTPL1 | Na3VO4 | FI |
| PTPN22 | PTPN8 | Na3VO4 | FI |
| PTPRB | PTPB | Na3VO4 | FI |
| PTPRC | CD45, LCA, T200, LY5, B220, GP180 | Na3VO4 | FI |
| PTPRE | / | Na3VO4 | FI |
| PTPRM | PTPμ | Na3VO4 | FI |
| DUSP3 | VHR | Na3VO4 | FI |
| DUSP10 | MKP5 | Na3VO4 | FI |
| DUSP13 | TMDP | Na3VO4 | FI |
| DUSP22 | JKAP, JSP1, MKPX | Na3VO4 | FI |
| PTEN | MMAC1, TEP1 | BpV(Hopic) | FI |
| LMPTP-A | ACP1 | Na3VO4 | FI |
| LMPTP-B | HCPTP-B | Na3VO4 | FI |
| CDC25A | / | Na3VO4 | FI |
| CDC25B | CDC25HU2 | Na3VO4 | FI |
| CDC25C | / | Na3VO4 | FI |
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