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Inhibition of human recombinant C-terminal FLAG-tagged SMS2 expressed in Freestyle293 cell membrane using C14-phosphatidylcholineD72 and C17-ceramide pre-incubated for 60 mins followed by incubation with substrate for 30 mins measured by RapidFire/MS assay
Assay data:16 Active, 14 Activity ≤ 1 µM, 17 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of SMS2 in human HuH7 cells assessed as down regulation of apoB secretion incubated for 17 hrs followed by further incubation for 2 hrs in presence of [35S]-methionine
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of purified SMS2 (unknown origin) using C6-NBD-Ceramide and DMPC as substrates preincubated for 5 mins followed by substrate addition and measured after 30 mins by TLC or HPLC method
Assay data:1 Active, 1 Activity ≤ 1 µM, 2 Tested
Inhibition of SMS2 (unknown origin) over-expressed in H5 insect cell lysate using C6-NBD-Ceramide and DMPC as substrates preincubated for 30 mins followed by substrate addition and measured after 2 hrs by TLC or HPLC method
Assay data:25 Active, 11 Activity ≤ 1 µM, 39 Tested
Inhibition of SMS2 (unknown origin) over-expressed in H5 insect cell lysate at 100 uM using C6-NBD-Ceramide and DMPC as substrates preincubated for 30 mins followed by substrate addition and measured after 2 hrs by TLC or HPLC method relative to control
Assay data:6 Tested
Noncompetitive inhibition of SMS2 (unknown origin) stably expressed in mouse ZS cells using 5 to 50 uM C6-NBD-ceramide as substrate preincubated for 30 mins followed by substrate addition and measured after 3 hrs by HPLC analysis
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
Inhibition of SMS2 (unknown origin) stably expressed in mouse ZS cells using C6-NBD-ceramide as substrate preincubated for 30 mins followed by substrate addition and measured after 3 hrs by HPLC analysis
Assay data:4 Active, 4 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of SMS2 (unknown origin)
Assay data:1 Active, 1 Tested
RNAi screen for vemurafenib enhancer genes in BRAFV600 melanoma - Primary Screen
Assay data:790 Active, 18119 Tested
Summary
Binding affinity to full length C-terminal FLAG tagged human SMS2 expressed in HEK293 cells at 500 to 1500 nM after 120 mins in presence of excess of N-(3,5-bis(trifluoromethyl)benzyl)-N,1-dimethyl-2-oxo-4-((2-phenylpyridin-4-yl)methoxy)-1,2-dihydroquinoline-3-carboxamide by AS/MS analysis
Time-dependent inhibition of full length C-terminal FLAG tagged human SMS2 expressed in HEK293 cell membranes using DMPC-d72 and C17-ceramide as substrate preincubated with enzyme followed by substrate addition by RapidFire/mass spectrometry assay
Inhibition of full length C-terminal FLAG tagged human SMS2 expressed in HEK293 cell membranes at 3 uM using DMPC-d72 and C17-ceramide as substrate preincubated for 60 mins followed by substrate addition measured after 30 mins by RapidFire/mass spectrometry assay
Assay data:3 Active, 3 Tested
Inhibition of human SMS2
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Reversible inhibition of full length C-terminal FLAG tagged human SMS2 expressed in HEK293 cells at 3 uM using DMPC-d72 and C17-ceramide as substrate preincubated for 60 mins followed by 33 fold diluted substrate addition measured after 30 mins by RapidFire/mass spectrometry assay relative to control
Inhibition of full length C-terminal FLAG tagged human SMS2 expressed in HEK293 cell membranes using DMPC-d72 and C17-ceramide as substrate preincubated for 60 mins followed by substrate addition measured after 15 mins by RapidFire/mass spectrometry assay
Inhibition of full length C-terminal FLAG tagged human SMS2 expressed in HEK293 cell membranes using DMPC-d72 and C17-ceramide as substrate after 15 mins by RapidFire/mass spectrometry assay
Inhibition of full length C-terminal FLAG tagged human SMS2 expressed in HEK293 cell membranes using DMPC-d72 and C17-ceramide as substrate preincubated for 60 mins followed by substrate addition measured after 30 mins by RapidFire/mass spectrometry assay
Assay data:2 Active, 2 Activity ≤ 1 µM, 3 Tested
Inhibition of human SMS2 expressed in HEK293T cells at 100 uM using C2-ceramide as substrate preincubated for 60 mins followed by substrate addition measured after 30 mins by RapidFire/mass spectrometry assay relative to control
Binding affinity to full length C-terminal FLAG tagged human SMS2 expressed in HEK293 cells after 120 mins by AS/MS analysis
Binding affinity to full length C-terminal FLAG tagged human SMS2 S227A mutant expressed in HEK293 cells after 120 mins by AS/MS analysis
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