Phosphatases are a superfamily of enzymes that hydrolyze the phosphate ester bond to remove phosphate groups from proteins, lipids, and nucleotides. As functional antagonists of protein kinases, they form the other half of the core cellular signaling regulatory network. Based on substrate specificity, phosphatases can be broadly categorized into:
- Serine/Threonine Protein Phosphatases (Ser/Thr PPs): In this class, PP1, PP2A, PP2B, PP2C, are the major Ser/Thr PPs which predominantly catalyze their reactions through a metal-dependent mechanism and are key regulators of metabolism, cell cycle, and signal transduction.
- Classical Protein Tyrosine Phosphatases (PTPs): Utilize a catalytic cysteine as the nucleophile to specifically dephosphorylate phosphotyrosine residues.
- Dual-Specificity Phosphatases (DUSPs): Capable of dephosphorylating both serine/threonine and tyrosine residues (e.g., DUSP22).
- Lipid Phosphatases: Such as PTEN, which regulate the PI3K/AKT pathway.
- Low Molecular Weight Phosphatases (LMW-PTPs/ACP1): Which are structurally more compact and with their own unique substrate specificities.
Role of phosphatases in drug discovery
Phosphatases fine-tune signaling thresholds in feedback loops and pathway crosstalk which enables them to control various pathological processes such as tumor immune evasion and metabolic diseases along with inflammation, fibrosis and neurodegeneration. PTP1B is a prototypical dual target in metabolic disease and oncology, SHP2 (PTPN11) has emerged as an oncotarget and master node of the RAS/MAPK pathway, and PTEN is the archetypal tumor suppressor. In all, phosphatases have recently emerged as a set of interesting drug targets, with drugs in various stages of development, including inhibitors, allosteric modulators, reversible and irreversible covalent inhibitors, and even targeted protein degraders (e.g., molecular glue or PROTAC approaches).
Our Phosphatase Screening Services
Creative Bioarray's Phosphatase Screening Services are designed to provide efficient and high-throughput in vitro activity assessment to accelerate your drug discovery programs. We offer comprehensive phosphatase activity assays and inhibitor screening to help you rapidly identify and optimize potential therapeutic candidates.
Fluorescence-based phosphatase activity assay:
We utilize a fluorescence-based phosphatase activity assay employing the fluorogenic substrate DiFMUP (6,8-difluoro-4-methylumbelliferyl phosphate). While DiFMUP itself is non-fluorescent, enzymatic dephosphorylation releases DiFMU (6,8-difluoro-4-methylumbelliferone), a highly fluorescent product that emits at 460 nm upon excitation at 355 nm. By continuously monitoring changes in fluorescence intensity, we can accurately quantify phosphatase activity and evaluate compound-mediated inhibition.
Key advantages of this assay include:
- High sensitivity with low background signal
- Robust scalability for high-throughput screening
- Real-time kinetic measurements for mechanistic insights
- Excellent compatibility with large compound library screening
Why Choose Our Phosphatase Screening Services?
Flexible service options
- Primary screening (single-concentration format)
- Dose–response profiling (multi-point IC₅₀ curves)
- Mechanistic studies (enzyme kinetics, inhibition modes)
- Selectivity profiling across phosphatase family members
Advanced technology platform
- High-throughput assay formats (384-well standard, 1536-well available on request)
- Automated liquid handling for precision and reproducibility
- State-of-the-art fluorescence detection systems for optimal assay sensitivity
Customized solutions
- Substrate optimization for challenging or atypical phosphatases
- Tailored buffer conditions to accommodate redox sensitivity or metal ion requirements
- Adaptable workflows to integrate with downstream assays or mechanistic studies
Our Phosphatase Screening Services provide high-quality, reproducible data to advance your drug discovery pipeline from hit identification through lead optimization. With broad target coverage, flexible service options, and deep scientific expertise, we are positioned to support your program at every stage of development.
Our customer service representatives are available 24 hours a day, 7 days a week.
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