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Inhibition of Sprague-Dawley rat brain microsome HO-2 assessed as bilirubin formation incubated for 60 mins by double-beam spectrophotometry
Assay data:4 Active, 2 Activity ≤ 1 µM, 24 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Heme Oxygenase from Article 10.1111/j.1747-0285.2009.00909.x: "Heme oxygenase inhibition by 2-oxy-substituted 1-azolyl-4-phenylbutanes: effect of variation of the azole moiety. X-ray crystal structure of human heme oxygenase-1 in complex with 4-phenyl-1-(1H-1,2,4-triazol-1-yl)-2-butanone."
Assay data:4 Active, 1 Activity ≤ 1 µM, 57 Tested
In Vitro HO Activity Assay from Article 10.1124/jpet.106.102699: "Inhibition of the enzymatic activity of heme oxygenases by azole-based antifungal drugs."
Assay data:5 Active, 2 Activity ≤ 1 µM, 9 Tested
In Vitro HO Activity Assay from Article 10.1016/j.bmc.2009.01.078: "Synthesis and evaluation of imidazole-dioxolane compounds as selective heme oxygenase inhibitors: effect of substituents at the 4-position of the dioxolane ring."
Assay data:30 Active, 8 Activity ≤ 1 µM, 35 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Covalent binding affinity to HMOX2 at Cys282 residue in human NCI-H358 cells assessed as reduction of log2 H/L ratio for tryptic peptide GALEGSSCPFR incubated for 4 hrs followed by cell lysis and subsequently labelled with light thiol probe N-((S)-18-iodo-11-isopropyl-10,13,17-trioxo-3,6-dioxa-9,12,16-triazaoctadecyl)-6-((4R,5S)-5-methyl-2-oxoimidazolidin-4-yl)hexanamide and heavy thiol probe 4 for 1 hr under dark conditions followed by tryptic digestion for overnight and measured by discovery ABPP based nano LC-MS/MS analysis
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Covalent binding affinity to HMOX2 at Cys282 residue in human NCI-H358 cells assessed as log2 H/L ratio at 10 uM pretreated for 3 hrs followed by N-(((6S,7R)-7-(4-chloro-3-fluorophenyl)-1,4-oxazepan-6-yl)methyl)-2-hydroxyacetamide treatment for 3 hrs by competitive TMT click chemistry pull-down experiment based LC-MS/MS analysis
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Binding affinity to HMOX2 in human HePAD38 cells infected with HBV assessed as protein labelling at 20 uM after 1 hr by photoaffinity labelling in-situ fluorescence gel-based LC-MS/MS analysis
Inhibition of HO-2 in Sprague-Dawley rat brain microsomes using NADPH as substrate incubated for 60 mins by spectrometry based assay
Inhibition of HO-2 in Sprague-Dawley rat brain microsomes using NADPH as substrate preincubated for 10 mins followed by substrate addition and measured after 15 mins by GC analysis
Assay data:6 Active, 9 Tested
Inhibition of recombinant truncated HO-2 (Met1 to Ala288) in rat brain microsomes expressed in Escherichia coli by spectrometry based assay
Inhibition of HO-2 (unknown origin)
Assay data:2 Active, 1 Activity ≤ 1 µM, 4 Tested
Activation of rat brain microsome HO-2 expressed in Escherichia coli BL21 (DE3) cells preincubated for 10 mins followed by NADPH addition and measured after 15 mins by gas chromatography relative to control
Assay data:6 Tested
Inhibition of Sprague-Dawley rat brain microsome HO-2 preincubated for 10 mins followed by beta-NADPH addition and measured after 15 mins by gas chromatography
Assay data:34 Active, 3 Activity ≤ 1 µM, 35 Tested
Inhibition of rat brain microsome HO-2 preincubated for 10 mins followed by beta-NADPH addition and measured after 15 mins by gas chromatography
Assay data:2 Active, 2 Tested
Binding affinity to HMOX2 in human A549 cells lysates grown on SILAC media at 10 uM incubated for 1 hr by LC-MS/MS analysis relative to untreated control
Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.
Assay data:1 Active, 1 Activity ≤ 1 µM, 236 Tested
Binding affinity to HMOX2 cysteine residue in human 786-O cell lysate at 5 uM incubated for 1 hr followed by cell lysis by IA-alkyne probe based isoTOP-ABPP analysis
Binding affinity to HMOX2 cysteine residue in human 786-O cell soluble proteomic lysate at 5 uM incubated for 1 hr followed by cell lysis by IA-alkyne probe based isoTOP-ABPP analysis
Assay data:3 Active, 3 Tested
Inhibition of HO-2 in Sprague-Dawley albino rat brain microsomes assessed as reduction in bilirubin formation using hemin as substrate after 60 mins in presence of NADPH by biliverdin reductase enzyme coupled spectrophotometric assay
Assay data:5 Active, 5 Activity ≤ 1 µM, 25 Tested
Rat Haem oxygenase 2 (Haem oxygenase)
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