Representative results from PhosphataseProfiler screening of six compounds against a panel of phosphatases shows targeted inhibition of PP1a, PP1b, and PP2A.
PhosphataseProfiler Service
Protein phosphatases are rising in interest as a relevant, druggable target class. As with kinases, inhibitor specificity is a major challenge for discovery scientists. PhosphataseProfiler, Millipore’s phosphatase specificity testing service, offers a robust and convenient way to rapidly generate inhibition profiles for phosphatase inhibitors.
Reversible protein phosphorylation is a key component of cellular regulation and homeostasis, controlling numerous biological processes including gene transcription, insulin signaling and synaptic transmission.
PhosphataseProfiler Highlights:
Single point inhibition data or 10-point IC50 curves
A panel of 21 protein phosphatases for selectivity profiling of novel chemical entities
Easy addition of any number of phosphatases to your KinaseProfiler project
Turnaround: 2 weeks or less
Targets Available in PhosphataseProfiler
CD45
PTP MEG1
DUSP22
PTP MEG2
HePTP
PTPN22
LMPTP-A
RPTPµ
LMPTP-B
SHP-1
MKP5
SHP-2
PP1α
TCPTP
PP2A
TMDP
PP5
VHR
PTP-1B
YopH
PTPβ
DiFMUP Phosphatase Assay Principle
Millipore’s PhosphataseProfiler assay utilizes DiFMUP (Molecular Probes) – 6,8-difluoro-4-methylumbelliferyl phosphate – as a universal substrate. This molecule has low fluorescence intensity in its non-hydrolyzed form. Removal of the phosphate group yields a highly fluorescent product.