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In Vitro Biochemical Evaluation from US Patent US10308663: "Inhibitors of PTP4A3 for the treatment of cancer"
Assay data:2 Active, 2 Activity ≤ 1 µM, 3 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Inhibition of recombinant human PTP4A3
Assay data:7 Active, 3 Activity ≤ 1 µM, 7 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of PRL-3 in human SW480 cells assessed as total KRT8 expression level at 5 to 50 uM by Western blot analysis
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of PRL-3 in human SW480 cells assessed as total Ezrin expression level at 5 to 50 uM by Western blot analysis
Inhibition of PRL-3 in human SW480 cells assessed as increase in phosphorylation of KRT8 at S431 at 5 to 50 uM by Western blot analysis
Inhibition of PRL-3 in human SW480 cells assessed as increase in phosphorylation of Ezrin at Thr567 at 5 to 50 uM by Western blot analysis
Inhibition of PRL-3 in human SW480 cells assessed as increase in phosphorylation of KRT8 at S73 at 5 to 50 uM by Western blot analysis
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of PRL-3 in human SW480 cells assessed as increase in phosphorylation of Ezrin at Tyr353 at 5 to 50 uM by Western blot analysis
Binding affinity to PRL-3 (unknown origin) at molar ratio of 1:1 by fluorescence spectroscopy
Assay data:6 Tested
Binding affinity to PRL-3 (unknown origin) assessed as quenching constant by Stern-Volmer plot analysis
Inhibition of PRL-3 (unknown origin) using DiFMUP as substrate incubated for 5 mins
Inhibition of recombinant human His6-tagged PRL-3 expressed in Escherichia coli using DiFMUP as substrate incubated for 30 mins by fluorescence based assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Inhibition of PRL-3 (unknown origin) using DiFMUP as substrate incubated for 1 hr
Inhibition of human brain PRL-3 (1 to 168 residues) expressed in Escherichia coli BL21(DE3) cells using DiFMUP as substrate incubated for 1 hr by fluorimetric assay
Assay data:2 Tested
Inhibition of full-length human heart His6-tagged PRL-3 expressed in Escherichia coli using DiFMUP as substrate incubated for 35 mins by fluorescence based assay
Inhibition of recombinant human His-6-tagged PTP4A3 expressed in Escherichia coli assessed as reduction in hydrolysis using DIFMUP as substrate incubated for 30 mins in presence of DTT by Fluorescence based method
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Inhibition of recombinant human His-6-tagged PTP4A3 expressed in Escherichia coli assessed as increase in polarization using TAMRAThr-Ala-Asp-Ile-Tyr(PO3H2)-Glu-NH2 as substrate by IMAP-FP assay
Inhibition of recombinant human PTP4A3 expressed in Escherichia coli BL21 (DE3) assessed as reduction in hydrolysis using DIFMUP as substrate incubated for 5 mins in presence of DTT
Assay data:3 Tested
Inhibition of PTP4A3 (unknown origin)
Oxidation of 15N-labeled reduced human PRL3 assessed as appearance of oxidized PRL3 signal peak at 0.25 mM by 15N-1H NMR spectroscopy relative to 7-amino-2-phenyl-5H-thieno[3,2-c]pyridin-4-one
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