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Inhibition of human immunoproteasome beta5 subunit using Suc-RLR-AMC as substrate pretreated for 30 mins followed by substrate addition and measured after 60 mins by fluorescence assay
Assay data:6 Active, 6 Activity ≤ 1 µM, 7 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of 20S proteasome beta2 subunit in human Jurkat cell lysate using Suc-RLR-AMC as substrate pretreated for 30 mins followed by substrate addition and measured after 60 mins by fluorescence assay
Assay data:17 Active, 3 Activity ≤ 1 µM, 18 Tested
Cytotoxicity against human RPMI8226 cells after 48 hrs by MTT assay
Assay data:22 Active, 14 Activity ≤ 1 µM, 26 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay
Assay data:21 Active, 14 Activity ≤ 1 µM, 26 Tested
Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
Assay data:22 Active, 10 Activity ≤ 1 µM, 27 Tested
Inhibition of yeast 20S proteasome beta5 subunit using Suc-LLVY-AMC as substrate pretreated for 30 mins followed by substrate addition and measured after 60 mins by fluorescence assay
Assay data:7 Active, 7 Activity ≤ 1 µM, 7 Tested
Inhibition of yeast 20S proteasome beta2 subunit using SUC-RLR-AMC as substrate pretreated for 30 mins followed by substrate addition and measured after 60 mins by fluorescence assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 7 Tested
Inhibition of yeast 20S proteasome beta1 subunit using fluorescent substrate pretreated for 30 mins followed by substrate addition and measured after 60 mins by fluorescence assay
Assay data:4 Active, 2 Activity ≤ 1 µM, 7 Tested
Inhibition of 20S proteasome beta5 subunit in human Jurkat cell lysate using Suc-LLVY-AMC as substrate pretreated for 30 mins followed by substrate addition and measured after 60 mins by fluorescence assay
Assay data:26 Active, 26 Activity ≤ 1 µM, 26 Tested
Binding affinity to 20S proteasome beta5 subunit in human Jurkat cell lysate assessed as decrease in protein hydrolysis at 100 uM pretreated for 30 mins followed by Suc-LLVY-AMC addition and measured after 1 hr by fluorescence assay
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Half life in 0.1 M TEAA buffer by RP-HPLC analysis
Assay data:1 Tested
SummaryPubMed Citation
Half life in human AB serum by RP-HPLC analysis
n-Octanol/Tris-HCl buffer partition coefficient, log P of the compound at 0.5 mg after 2 mins by RP-HPLC method
Inhibition of 20S proteasome beta5 subunit in human MCF7 cells using Suc-LLVY-AMC as substrate pretreated for 1 hr followed by compound washout and cell lysis prior to substrate addition measured after 1 hr by fluorescence assay
Assay data:9 Active, 14 Tested
Cell cycle arrest in human Jurkat cells assessed as accumulation at G2/M phase at 0.1 to 1 uM after 10 hrs by Vybrant DyeCycle Orange staining based flow cytometry
Assay data:2 Active, 2 Tested
SummaryCompounds, ActivePubMed Citation
Induction of apoptosis in human Jurkat cells after 24 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry
Inhibition of 20S proteasome beta5 subunit in human MCF7 cells assessed as accumulation of ubiuitinated protein at 1 to 10 uM after 9.5 hrs by Western blot analysis
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