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Proteasome Inhibitory Activity from US Patent US11542283: "Synthesis of peptide borate ester compound and use thereof"
Assay data:8 Active, 8 Activity ≤ 1 µM, 8 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Activation of human 20S proteosome at chymotrypsin like site assessed as maximum fold change in substrate degradation using Suc-LLVY-AMC as flurogenic substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by spectrometric analysis relative to control
Assay data:7 Tested
SummaryPubMed CitationRelated BioAssays by Target
Activation of human 20S proteosome at chymotrypsin like site assessed as substrate degradation using Suc-LLVY-AMC as flurogenic substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by spectrometric analysis
Assay data:7 Active, 1 Activity ≤ 1 µM, 17 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Activation of human 20S proteosome at trypsin-like site assessed as maximum fold change in substrate degradation using Boc-LLR-AMC as flurogenic substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by spectrometric analysis relative to control
Assay data:8 Tested
Activation of human 20S proteosome at trypsin-like site assessed as substrate degradation using Boc-LLR-AMC as flurogenic substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by spectrometric analysis
Activation of human 20S proteosome at caspase-like site assessed as maximum fold change in substrate degradation using Z-LLE-AMC as flurogenic substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by spectrometric analysis relative to control
Assay data:6 Tested
Activation of human 20S proteosome at caspase-like site assessed as substrate degradation using Z-LLE-AMC as flurogenic substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by spectrometric analysis
Assay data:6 Active, 17 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Activation of human 20S proteosome assessed as maximum fold change in substrate degradation using Suc-LLVY-AMC/Z-LLE-AMC/Boc-LLR-AMC as flurogenic substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by spectrometric analysis relative to control
Assay data:9 Tested
Activation of human 20S proteosome assessed as substrate degradation using Suc-LLVY-AMC/Z-LLE-AMC/Boc-LLR-AMC as flurogenic substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by spectrometric analysis
Inhibition of chymotrypsin-like activity of 20S proteasome in human MM1.S cells assessed as accumulation of polyubiquitinated proteins at 10 to 1000 nM and measured by Western blot analysis
Assay data:3 Active, 3 Tested
Inhibition of chymotrypsin-like activity of human 20S proteasome using Suc-Leu Leu-Val-Tyr-AMC as substrate preincubated for 15 mins followed by substrate addition measured by fluorescence assay
Assay data:25 Active, 1 Activity ≤ 1 nM, 22 Activity ≤ 1 µM, 34 Tested
Inhibition of human 20s proteasome
Assay data:11 Tested
Inhibition of chymotrypsin-like activity of human erythrocytes 20S proteasome using Suc-LLVY-AMC as substrate and measured by fluorescence assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Inhibition of human 20S proteasome chymotrypsin-like activity at 11 uM using Succ-Leu-Leu-Val-Tyr-AMC as fluorogenic substrate by fluorometric assay
Inhibition of human 20S proteasome caspase-like activity at 11 uM using Cbz-Leu-Leu-Glu-AMC as fluorogenic substrate by fluorometric assay
Inhibition of human 20S proteasome trypsin-like activity at 11 uM using Boc-Leu-Arg-Arg-AMC as fluorogenic substrate by fluorometric assay
Inhibition of 20S proteasome (unknown origin) by fluorescence based assay
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Activation of human 20S proteasome mediated degradation of alpha-synuclein assessed as amount of alpha-synuclein remaining at 25 uM and incubated for 2 hrs by Coomassie staining based SDS-PAGE analysis
Assay data:4 Active, 4 Tested
Stimulation of human 20S proteasome assessed as increase in proteasome activity at 25 uM and measured upto 60 mins using FRET peptide as substrate by FRET assay relative to control
Assay data:29 Tested
Proteasome Activity Assay from Article 10.1021/acschembio.7b00489: "Small Molecule Enhancement of 20S Proteasome Activity Targets Intrinsically Disordered Proteins."
Assay data:5 Active, 13 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
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