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Literature summary for 2.3.1.B41 extracted from

  • Kokkonen, P.; Rahnasto-Rilla, M.; Mellini, P.; Jarho, E.; Lahtela-Kakkonen, M.; Kokkola, T.
    Studying SIRT6 regulation using H3K56 based substrate and small molecules (2014), Eur. J. Pharm. Sci., 63, 71-76.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(4R)-1-[(benzyloxy)carbonyl]-4-hydroxy-L-prolyl-N6-ethanethioyl-N-phenyl-L-lysinamide 0.2 mM, 56% inhibition, substrate: Ac-RYQ(N6-acetyl)K-7-amido-4-methylcoumarin Homo sapiens
1-(tert-butoxycarbonyl)-L-prolyl-N6-ethanethioyl-N-phenyl-L-lysinamide 0.2 mM, 32% inhibition, substrate: Ac-RYQ(N6-acetyl)K-7-amido-4-methylcoumarin Homo sapiens
6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide i.e. EX-527. 0.2 mM, 56% inhibition, substrate: Ac-RYQ(N6-acetyl)K-7-amido-4-methylcoumarin Homo sapiens
methyl N2-acetyl-N6-ethanethioyl-L-lysyl-L-alaninate 0.2 mM, 20% inhibition, substrate: Ac-RYQ(N6-acetyl)K-7-amido-4-methylcoumarin Homo sapiens
N2-[(benzyloxy)carbonyl]-N6-ethanethioyl-N-(2-fluorophenyl)-L-lysinamide 0.2 mM, 25% inhibition, substrate: Ac-RYQ(N6-acetyl)K-7-amido-4-methylcoumarin Homo sapiens
N2-[(benzyloxy)carbonyl]-N6-ethanethioyl-N-pyridin-3-yl-L-lysinamide 0.2 mM, 54% inhibition, substrate: Ac-RYQ(N6-acetyl)K-7-amido-4-methylcoumarin Homo sapiens
N2-[(benzyloxy)carbonyl]-N6-ethanethioyl-N-[2-(4-methoxyphenyl)-2-oxoethyl]-L-lysinamide 0.2 mM, 48% inhibition, substrate: Ac-RYQ(N6-acetyl)K-7-amino-4-methylcoumarin Homo sapiens
N6-ethanethioyl-N-(2-oxo-2-phenylethyl)-N2-(3-phenylpropanoyl)-L-lysinamide 0.2 mM, 20% inhibition, substrate: Ac-RYQ(N6-acetyl)K-7-amido-4-methylcoumarin Homo sapiens
N6-ethanethioyl-N-phenyl-N2-[3-(pyridin-3-yl)propanoyl]-L-lysinamide 0.2 mM, 18% inhibition, substrate: Ac-RYQ(N6-acetyl)K-7-amido-4-methylcoumarin Homo sapiens
N6-ethanethioyl-N2-(3-phenylpropanoyl)-L-lysyl-L-alanine 0.2 mM, 20% inhibition, substrate: Ac-RYQ(N6-acetyl)K-7-amido-4-methylcoumarin Homo sapiens
N6-ethanethioyl-N2-[3-(2-fluorophenyl)propanoyl]-N-pyridin-3-yl-L-lysinamide 0.2 mM, 58% inhibition, substrate: Ac-RYQ(N6-acetyl)K-7-amino-4-methylcoumarin Homo sapiens
quercetin 0.2 mM, 52% inhibition, substrate: Ac-RYQ(N6-acetyl)K-7-amido-4-methylcoumarin Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q8N6T7
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
NAD+ + Ac-AK(N6-acetyl)K-7-amido-4-methylcoumarin the substrate is based on the human tumour suppressor protein p53 Homo sapiens nicotinamide + Ac-AKK-7-amido-4-methylcoumarin + 2'-O-acetyl-ADP-ribose
-
?
NAD+ + Ac-HK(N6-acetyl)K-7-amido-4-methylcoumarin the substrate is based on the human tumour suppressor protein p53 Homo sapiens nicotinamide + Ac-HKK-7-amido-4-methylcoumarin + 2'-O-acetyl-ADP-ribose
-
?
NAD+ + Ac-RHK(N6-acetyl)K-7-amido-4-methylcoumarin the substrate is based on the amino acids 379-382 of the human tumour suppressor protein p53 Homo sapiens nicotinamide + Ac-RHKK-7-amido-4-methylcoumarin + 2'-O-acetyl-ADP-ribose
-
?
NAD+ + Ac-RYQ(N6-acetyl)K-7-amido-4-methylcoumarin the peptide substrate mimics the biological deacetylation site of histone H3 K56 Homo sapiens nicotinamide + Ac-RYQK-7-amido-4-methylcoumarin + 2'-O-acetyl-ADP-ribose
-
?
NAD+ + Ac-TAR(N6-acetyl)K-7-amido-4-methylcoumarin the peptide substrate mimics the biological deacetylation site of histone H3 K9 Homo sapiens nicotinamide + Ac-TARK-7-amido-4-methylcoumarin + 2'-O-acetyl-ADP-ribose
-
?

Synonyms

Synonyms Comment Organism
SIRT6
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens