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Inhibition of ERCC1-XPF in UV-radiated human HCT-116 cells assessed as cyclobutane pyrimidine dimer DNA repair at 2 uM preincubated for 1 hr followed by 8 J/m2 UV-C radiation and measured up to 24 hrs by IgG-Alexafluor antibody based fluorescent microscopic analysis (Rvb = 16%)
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Binding affinity to His-tagged human ERCC1-XPF expressed in Escherichia coli BL21 (DE3) cells at 4 uM by steady-state fluorescence assay relative to control
Assay data:2 Tested
Inhibition of human His-tagged ERCC1-XPF expressed in Escherichia coli BL21 (DE3) cells using 6-FAM-5'CAGCGCTCGG(20T)CCGAGCGCTG-3'-dabcyl at 10 uM measured for 12 mins by fluorescence incision assay
Assay data:8 Active, 12 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Binding affinity to His-tagged human ERCC1-XPF expressed in Escherichia coli BL21 (DE3) cells by steady-state fluorescence assay
Assay data:2 Active, 2 Activity ≤ 1 µM, 3 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of human His-tagged human ERCC1-XPF expressed in Escherichia coli BL21 (DE3) cells using 6-FAM-5'CAGCGCTCGG(20T)CCGAGCGCTG-3'-dabcyl measured for 12 mins by fluorescence incision assay
Assay data:2 Active, 1 Activity ≤ 1 µM, 3 Tested
Inhibition of human His6-tagged ERCC1-XPF endonuclease activity expressed in Escherichia coli BL21 (DE3) using [6-FAM-5'-CAGCGCTCGG(20T)CCGAGCGCTG-3'-dabcyl] as substrate measured after 30 mins in presence of 5% DMSO by fluorescence assay
Assay data:2 Active, 1 Activity ≤ 1 µM, 2 Tested
Inhibition of ERCC1-XPF-mediated nucleotide excision repair in human HCT116 cells assessed as reduction in removal of UV-induced cyclobutane pyrimidine dimer at 2 uM incubated for 1 hr prior to compound washout followed by 8 J/m2 UV irradiation and subsequent compound addition and measured after 24 hrs by DAPI staining-based immunofluorescence assay
Inhibition of ERCC1-XPF-mediated nucleotide excision repair in human HCT116 cells assessed as reduction in removal of UV-induced cyclobutane pyrimidine dimer by measuring cyclobutane pyrimidine dimer level at 2 uM incubated for 1 hr prior to compound washout followed by 8 J/m2 UV irradiation and subsequent compound addition and measured after 24 hrs by DAPI staining-based immunofluorescence assay (Rvb = 80%)
Binding affinity to human N-terminal His6-tagged RED-tris-NTA labelled ERCC1 (96 to 297 residues)-XPF (667 to 916 residues) expressed in Escherichia coli BL21 (DE3) at 10 uM measured after 20 mins by microscale thermophoresis assay
Assay data:1 Active, 1 Tested
Binding affinity to human His6-tagged ERCC1-XPF expressed in Escherichia coli BL21 (DE3) by spectrofluorimetric method
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Binding affinity to human His6-tagged ERCC1-XPF expressed in Escherichia coli BL21 (DE3) assessed as tryptophan fluorescence quenching at 2 uM by spectrofluorimetric method relative to control
Time dependent inhibition of human His6-tagged ERCC1-XPF endonuclease activity expressed in Escherichia coli BL21 (DE3) at 3 uM using [6-FAM-5'-CAGCGCTCGG(20T)CCGAGCGCTG-3'-dabcyl] as substrate in presence of 5 to 10% DMSO by fluorescence assay
Inhibition of human His6-tagged ERCC1-XPF endonuclease activity expressed in Escherichia coli BL21 (DE3) at 8 uM using [6-FAM-5'-CAGCGCTCGG(20T)CCGAGCGCTG-3'-dabcyl] as substrate measured for 12 mins by fluorescence assay
Assay data:3 Active, 4 Tested
RNAi screen for vemurafenib enhancer genes in BRAFV600 melanoma - Primary Screen
Assay data:790 Active, 18119 Tested
Summary
Inhibition of ERCC1-XPF in human A375 cells assessed as induction of delay in DNA repair by measuring cumulative frequency of cells up to 10 uM pre-incubated for 1 hr before cisplatin exposure for 1 hr by immunohistochemistry based gammaH2AX foci assay
Inhibition of ERCC1-XPF in human A375 cells assessed as potentiation of cisplatin-induced cytotoxicity at 0.1 to 3 uM incubated for 5 days
Inhibition of ERCC1-XPF in human A375 cells assessed as reduction in direct nucleotide excision repair of UV-damaged pEGFP plasmid up to 10 uM incubated for 24 hrs by recombinant GFP reporter assay
Binding affinity to ERCC1-XPF (unknown origin) assessed as melting temperature by thermal shift assay
Binding affinity to ERCC1-XPF (unknown origin) by SPR assay
Inhibition of ERCC1-XPF (unknown origin) by high-throughput fluorescence based in-vitro endonuclease assay
Assay data:28 Active, 10 Activity ≤ 1 µM, 38 Tested
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