Inhibition of ENTPD5 in PTEN knockout mouse MEF cells assessed as induction of ER stress by measuring increase in GRP78/BiP expression at 30 uM incubated for 24 hrs by Western blotting analysis
Antitumor activity against human LNCAP cells xenografted in mouse assessed as induction of tumor shrinkage at 1 to 100 mg/kg, ip dosed every other day and measured after 6 weeks by microscopy
Antitumor activity against human LNCAP cells xenografted in mouse assessed as reduction in cells left in matrigels at 1 to 100 mg/kg, ip dosed every other day and measured after 6 weeks by hematoxylin and eosin staining based microscopy
Inhibition of human recombinant ENTPD5 expressed in insect cells assessed as reduction in UDP hydrolysis at 1 uM incubated for 1 hr in presence of UMP, GTP and ATP by Escherichia coli UMP kinase pyrH catalyzed UMP phosphorylation coupled luciferase assay
Inhibition of human recombinant ENTPD5 expressed in insect cells assessed as reduction in UDP hydrolysis up to 10 uM incubated for 1 hr in presence of UMP, GTP and ATP by Escherichia coli UMP kinase pyrH catalyzed UMP phosphorylation coupled luciferase assay
Inhibition of recombinant Escherichia coli UMP kinase pyrH catalyzed UMP phosphorylation in presence of GTP and ATP incubated for 1 hr by luminescence based assay
Inhibition of human recombinant ENTPD5 expressed in insect cells assessed as reduction in reduction in UDP hydrolysis by measuring inorganic phosphate release incubated for 1 hr by malachite green based assay