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Assay Method Information

Assay Name:  In vitro MKP-1 Phosphatase Dose Response Active/Probe Assessment Assay - Effects of DTT
Description:  The MKP-1 dose response Active/Probe assessment-DTT assay has been developed to evaluate the effects of increased DTT concentration on the MKP-1 inhibition of actives identified in the MH-76391 In vitro MKP-1 HTS assay AID #374, and subsequently confirmed in the HTS dose response confirmation assay AID #551. Protein tyrosine phosphatases have an active site cysteine that is very susceptible to inactivation by oxidation. In addition, a number of compounds such as quinone-like compounds are capable of generating reactive oxygen species via redox cycling in the presence of DTT. Increasing the concentration of DTT from 1 mM to 25 mM does not affect the activity of MKP-1 in the assay but can reverse the inhibition of some inhibitors or significantly increase their IC50 values. The MKP-1 Phosphatase Dose Response Active/Probe Assessment Assay-Effects of DTT has been Developed and Run at the University of Pittsburgh Molecular Screening Center (PMLSC) part of the Molecular Library Screening
Affinity data for this assay
 

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Last update November 1, 2007
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