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Binding affinity to PRC2 complex of EZH2-EED-SUZ12 (unknown origin) assessed as dissociation constant by isothermal titration calorimetry method
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryRelated BioAssays by Target
Inhibition of PRC2 (unknown origin) using H3K27me0 as peptide substrate by LC-MS based analysis
Summary
Inhibition of His tagged EED (1 to 441) (unknown origin) using biotin-H3K27me3 peptide as substrate by AlphaScreen competition binding assay
Antiproliferative activity against human KARPAS-422 cells expressing EZH2 mutant assessed as inhibition of cell growth after 14 days by beckman coulter counting method
Assay data:5 Active, 3 Activity ≤ 1 µM, 5 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Inhibition of PRC2 in human G-401 cells assessed as H3K27 methylation status incubated for 48 hrs by ELISA method
Assay data:4 Active, 3 Activity ≤ 1 µM, 8 Tested
Inhibition of PRC2 (unknown origin) assessed as reduction in H3K27 trimethylation using H3K27Me0 peptide (21 to 44 residues) as substrate by measuring SAH formation by LC-MS analysis
Assay data:10 Active, 9 Activity ≤ 1 µM, 15 Tested
Antiproliferative activity against human KARPAS-422 cells expressing EZH2 Y641N mutant incubated for 14 days
Inhibition of PRC2 HMTase activity in human G-401 cells using nucleosome core particles as substrate in presence of activation peptide H3K27me3 (21 to 44 residues)
Inhibition of EED (unknown origin)
Assay data:15 Active, 14 Activity ≤ 1 µM, 15 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of full length N-terminal His-6x tagged EED (1 to 441 residues) (unknown origin) incubated for 1 hr by TR-FRET assay
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
TR-FRET Assay from US Patent US11013745: "Triazolopyrimidine, triazolopyridine compounds, and the composition thereof for treating PRC2-mediated diseases"
Assay data:79 Active, 79 Activity ≤ 1 µM, 79 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
HMT Assay from Article 10.1038/nchembio.2304: "An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED."
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Isothermal Titration Calorimetry (ITC) from Article 10.1038/nchembio.2304: "An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED."
PRC2 Biochemical Assay from Article 10.1038/nchembio.2304: "An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED."
Inhibition of biotinylated H3K27Me3 peptide (19 to 33 residues) binding to His-tagged EED (1 to 441 residues) (unknown origin) preincubated for 15 mins followed by H3K27Me3 addition and measured after 30 mins by alphascreen competition binding assay
Assay data:35 Active, 16 Activity ≤ 1 nM, 35 Activity ≤ 1 µM, 35 Tested
Growth inhibition of human KARPAS-422 cells assessed as cell growth incubated for 7 days by lactate dehydrogenase based WST-8 assay
Assay data:35 Active, 4 Activity ≤ 1 nM, 35 Activity ≤ 1 µM, 35 Tested
Displacement of UNC5114-biotin tracer ligand from N-terminal 6His-tagged EED (1 to 441 residues) (unknown origin) expressed in Escherichia coli Rosetta2 BL21(DE3)pLysS cells measured after 1 hr by TR-FRET analysis
Binding affinity to EED in PRC2 complex (unknown origin) using H3K27me0 (21 to 44 residue) peptide as substrate by LC-MS analysis
Growth inhibition of human KARPAS422 cells incubated for 7 days by WST8 assay
Assay data:35 Active, 1 Activity ≤ 1 nM, 28 Activity ≤ 1 µM, 35 Tested
Inhibition of EED ( 1 to 441 residues) (unknown origin) pre-incubated for 15 mins before biotin-H3K27me3 (19 to 33 residues) addition and further incubated for 30 mins by AlphaScreen.based EED-H3K27me3 peptide competition binding assay
Assay data:35 Active, 12 Activity ≤ 1 nM, 35 Activity ≤ 1 µM, 35 Tested
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