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Inhibition of PDK in human A-375 cells assessed as reduction in PDH phosphorylation at ser293 residue at 5 to 20 uM after 24 to 48 hrs
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
PDHK4(h) Kinase panel
Assay data:1 Tested
SummaryRelated BioAssays by Target
Inhibition of human recombinant PDHK4 co-complexed with porcine PDH at 30 uM using sodium pyruvate, coenzymeA and NAD as substrates preincubated with enzyme complex for 45 mins followed by substrates addition and further incubated for 90 mins in presence of ATP at Km concentration by spectrophotometric assay relative to control
Assay data:2 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of human recombinant PDHK4 co-complexed with porcine PDH using sodium pyruvate, coenzymeA and NAD as substrates preincubated with enzyme complex for 45 mins followed by substrates addition and further incubated for 90 mins in presence of ATP at Km concentration by spectrophotometric assay
Assay data:23 Active, 13 Activity ≤ 1 µM, 27 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of human recombinant PDHK4 assessed as reduction in substrate phosphorylation at 50 to 500 nM using ATP and Ulight-CKKSRGDYMTMQIG (IRS-1) incubated for 60 min by LANCE detection method
PDK Inhibition Assay from Article 10.1074/jbc.M113.533885: "Structure-guided development of specific pyruvate dehydrogenase kinase inhibitors targeting the ATP-binding pocket."
Assay data:6 Active, 3 Activity ≤ 1 µM, 8 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
PDHK4(h) Eurofins kinase panel
PDHK4(h) Eurofins Kinase panel
PDHK4(h) Millipore kinase panel
Inhibition of human PDHK4 co-complexed with porcine PDH using sodium pyruvate, coenzymeA and NAD as substrate at IC50 preincubated with enzyme complex for 45 mins followed by ATP addition and then later incubated with substrate for 90 mins by absorption spectrophotometric assay relative to control
Assay data:9 Tested
Inhibition of human PDHK4 co-complexed with porcine PDH using sodium pyruvate, coenzymeA and NAD as substrate preincubated with enzyme complex for 45 mins followed by ATP addition and then later incubated with substrate for 90 mins by absorption spectrophotometric assay
Assay data:2 Active, 16 Tested
Inhibition of human PDHK4 assessed as reduction in acetyl-coenzymeA formation at IC50 by RapidFire mass spectrometry relative to control
Inhibition of human PDHK4 assessed as reduction in acetyl-coenzymeA formation by RapidFire mass spectrometry
Assay data:3 Tested
Inhibition of recombinant human full length PDHK4 assessed as residual activity at 10 uM using KKKYHGHSMSDPGVSYRT as substrate incubated for 40 mins in presence of [gamma33P]ATP by scintillation counting based radiometry assay relative to control
Binding affinity to PDK4 (unknown origin) by isothermal titration calorimetry
Inhibition of recombinant human His-tagged PDK4 expressed in Escherichia coli using PDH E1 as substrate measured after 30 mins by Kinase-Glo luminescence assay
Assay data:3 Active, 1 Activity ≤ 1 µM, 4 Tested
Inhibition of recombinant human full length PDHK4 at 1 uM using KKKYHGHSMSDPGVSYRT as substrate incubated for 40 mins in presence of [gamma-33P]-ATP by scintillation counting method relative to control
Inhibition of PDHK4 (unknown origin) at 1 uM relative to control
Inhibition of PDHK in human DU145 cells assessed as reduction in PDHE1a phosphorylation at Ser293 residue incubated for 2 hrs by Western blot analysis
Inhibition of PDHK in human H1299 cells assessed as reduction in PDHE1a phosphorylation at Ser293 residue at 20 uM incubated for 2 hrs by Western blot analysis
Assay data:2 Active, 2 Tested
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