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KAT-8 Enzyme Assay from US Patent US11685732: "MYST family histone acetyltransferase inhibitors"
Assay data:3 Active, 398 Tested
SummaryCompounds, ActiveRelated BioAssays by DepositorRelated BioAssays by Target
Kat8 Assay from US Patent US11492346: "Benzisoxazole sulfonamide derivatives"
Assay data:36 Active, 18 Activity ≤ 1 µM, 52 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Selectivity interaction (HAT panel) EUB0000329a MYST1
Assay data:1 Tested
SummaryRelated BioAssays by Target
Inhibition of human MOF using AcCoA and H4 peptide as substrate incubated for 12 min at room temperature relative to control
Assay data:1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of human MOF using AcCoA and H4 peptide as substrate at 1 uM incubated for 12 min at room temperature relative to control
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of MOF (unknown origin)
Inhibition of MOF (unknown origin) at 100 uM
Inhibition of human MYST1 (unknown origin) up to 50 uM
RNAi screen for vemurafenib enhancer genes in BRAFV600 melanoma - Primary Screen
Assay data:790 Active, 18119 Tested
Summary
Inhibition of N-terminal His6-tagged KAT8 catalytic domain (125 to 458 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) assessed as inhibitor-acetylated enzyme complex using SGRGKGGKGLGKGGAKRHRK-NH2 as substrate after 5 mins in presence of Ac-CoA by fluorescence assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of N-terminal His6-tagged KAT8 catalytic domain (125 to 458 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) assessed as inhibitor-enzyme complex using SGRGKGGKGLGKGGAKRHRK-NH2 as substrate after 5 mins in presence of Ac-CoA by fluorescence assay
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Reversible inhibition of N-terminal His6-tagged KAT8 catalytic domain (125 to 458 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) at 0.75 to 10 times IC50 using SGRGKGGKGLGKGGAKRHRK-NH2 as substrate preincubated for 2 to 10 mins followed by substrate addition measured after 15 mins in presence of Ac-CoA by fluorescence assay
Inhibition of N-terminal His6-tagged KAT8 catalytic domain (125 to 458 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) up to 100 uM using histone substrate after 15 mins in presence of CoA by fluorescence assay
Inhibition of N-terminal His6-tagged KAT8 catalytic domain (125 to 458 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) at 250 uM using SGRGKGGKGLGKGGAKRHRK-NH2 as substrate after 5 mins in presence of Ac-CoA by fluorescence assay
Assay data:10 Active, 19 Tested
Inhibition of N-terminal His6-tagged KAT8 catalytic domain (125 to 458 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) at 200 uM using SGRGKGGKGLGKGGAKRHRK-NH2 as substrate after 5 mins in presence of Ac-CoA by fluorescence assay
Assay data:2 Active, 2 Tested
Competitive inhibition of N-terminal His6-tagged KAT8 catalytic domain (125 to 458 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) assessed as apparent Km for histone substrate at 10 uM using preincubated for 5 mins followed by varying levels of histone substrate addition measured after 15 mins in presence of AC-CoA by Michaelis-Menten plot analysis (Rvb = 20 +/- 3.5 uM)
Competitive inhibition of N-terminal His6-tagged KAT8 catalytic domain (125 to 458 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) assessed as apparent Km for histone substrate at 5 uM using preincubated for 5 mins followed by varying levels of histone substrate addition measured after 15 mins in presence of AC-CoA by Michaelis-Menten plot analysis (Rvb = 20 +/- 3.5 uM)
Competitive inhibition of N-terminal His6-tagged KAT8 catalytic domain (125 to 458 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) assessed as apparent Vmax for histone substrate at 10 uM using preincubated for 5 mins followed by varying levels of histone substrate addition measured after 15 mins in presence of AC-CoA by Michaelis-Menten plot analysis (Rvb = 11 +/- 0.5 pmol/min)
Competitive inhibition of N-terminal His6-tagged KAT8 catalytic domain (125 to 458 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) assessed as apparent Vmax for histone substrate at 5 uM using preincubated for 5 mins followed by varying levels of histone substrate addition measured after 15 mins in presence of AC-CoA by Michaelis-Menten plot analysis (Rvb = 11 +/- 0.5 pmol/min)
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