Phosphatases

Phosphatases

ChemDiv offers high throughput screening (HTS) service
Phosphatases research platform

• 23 protein assays depending on groups available

• LANCE TR-FRET as a platform.

• 4 phosphatase-focused libraries (Human Phosphatases Annotated Library, Receptor protein tyrosine phosphatases, Protein Tyrosine Phosphatase Non-receptor Type (PTPN) Targeted Library, Phosphatases library), 52K compounds in total

• Our support in compound selection based on your research project

• Screening from 10000 compound sets up to 300000 and more

• A quick start of your research project

• 25 years of experience

Although phosphatases have the reputation of notoriously difficult therapy targets, there are several drugs going through their clinical trials that target them: TNO155, an allosteric SHP2 inhibitor; trodusquemine, an allosteric PTP1B inhibitor; IFB-088, a PPP1R15A/PP1c inhibitor. Additionally, there are other ways in which they are clinically relevant: levels of acid phosphatase are monitored during prostate cancer treatment in order to evaluate its success, determining the presence level of alkaline phosphatase in the blood is a way of checking for liver inflammation. Possible future drug targets include PP2a and PTEN, mutations in which are signatures in a number of tumor groups.

SHP2 structure, sequence from the PDB

One of the standard methods for measuring phosphatase activity is LANCE TR-FRET:

• Eu antibodies with phosphorylated peptides participate in TR-FRET
• Phosphatase dephosphorylates peptides
• The TR-FRET signal weakens
• The loss of the signal is a measure of phosphatase activity

As part of our target-to-clinic approach, ChemDiv offers assays for all common phosphatase assays, which you can add into your shopping cart: acid phosphatase, alkaline phosphatase, protein tyrosine phosphatase and serine/threonine phosphatase, just pick from the list below:

• DUSP22
• PP1A, PP1B
• PP2alpha
• PP2Calpha, PP2Cgamma
• PTEN
• PTPN1 and other PTPNXs, like PTPN7
• PTPRA and other PTPRXs, like PTPRF
• SHIP1, SHIP2