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Literature summary extracted from

  • Basavapathruni, A.; Gureasko, J.; Porter Scott, M.; Hermans, W.; Godbole, A.; Leland, P.A.; Boriack-Sjodin, P.A.; Wigle, T.J.; Copeland, R.A.; Riera, T.V.
    Characterization of the enzymatic activity of SETDB1 and its 1 1 complex with ATF7IP (2016), Biochemistry, 55, 1645-1651.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.1.1.366 ATF7IP SETDB1 partner protein. SETDB1 and the SETDB1:ATF7IP complex efficiently catalyze both monomethylation and dimethylation of H3K9 peptide substrates. The activity of the binary complex is 4fold lower than SETDB1 alone Homo sapiens
2.1.1.368 ATF7IP SETDB1 partner protein. SETDB1 and the SETDB1:ATF7IP complex efficiently catalyze both monomethylation and dimethylation of H3K9 peptide substrates. The activity of the binary complex is 4fold lower than SETDB1 alone Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.1.1.366 0.39
-
 [histone H3 peptide 1-15]-N6,N6-dimethyl-L-lysine9 SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
2.1.1.366 0.43
-
 [histone H3 peptide 1-15]-N6,N6-dimethyl-L-lysine9 pH 7.6, 23°C Homo sapiens
2.1.1.366 0.52
-
 S-adenosyl-L-methionine substrate [histone H3 peptide 1-15]-N6,N6-dimethyl-L-lysine9, SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
2.1.1.366 0.66
-
 S-adenosyl-L-methionine substrate [histone H3 peptide 1-15]-N6,N6-dimethyl-L-lysine9, pH 7.6, 23°C Homo sapiens
2.1.1.368 0.28
-
 [histone H3 peptide 1-15]-L-lysine9 SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
2.1.1.368 0.41
-
 [histone H3 peptide 1-15]-L-lysine9 pH 7.6, 23°C Homo sapiens
2.1.1.368 0.41
-
 [histone H3 peptide 1-15]-N6-methyl-L-lysine9 SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
2.1.1.368 0.53
-
 S-adenosyl-L-methionine substrate [histoneH3 peptide 1-15]-L-lysine9, SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
2.1.1.368 0.54
-
 S-adenosyl-L-methionine substrate [histoneH3 peptide 1-15]-N6-methyl-L-lysine9, SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
2.1.1.368 0.56
-
 S-adenosyl-L-methionine substrate [histoneH3 peptide 1-15]-N6-methyl-L-lysine9, pH 7.6, 23°C Homo sapiens
2.1.1.368 0.59
-
 [histone H3 peptide 1-15]-N6-methyl-L-lysine9 pH 7.6, 23°C Homo sapiens
2.1.1.368 0.68
-
 S-adenosyl-L-methionine substrate [histoneH3 peptide 1-15]-L-lysine9, pH 7.6, 23°C Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
2.1.1.366 Homo sapiens Q15047
-
-
2.1.1.368 Homo sapiens Q15047 cf. EC 2.1.1.366
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.1.1.366 additional information H3K9 methylation by SETDB1 occurs in a distributive manner Homo sapiens ?
-
 ?
2.1.1.366 S-adenosyl-L-methionine + [histone H3 peptide 1-15]-L-lysine9
-
 Homo sapiens S-adenosyl-L-homocysteine + [histone H3 peptide 1-15]-N6-methyl-L-lysine9
-
 ?
2.1.1.366 S-adenosyl-L-methionine + [histone H3 peptide 1-15]-N6,N6-dimethyl-L-lysine9
-
 Homo sapiens S-adenosyl-L-homocysteine + [histone H3 peptide 1-15]-N6,N6,N6-trimethyl-L-lysine9
-
 ?
2.1.1.366 S-adenosyl-L-methionine + [histone H3 peptide 1-15]-N6-methyl-L-lysine9
-
 Homo sapiens S-adenosyl-L-homocysteine + [histone H3 peptide 1-15]-N6,N6-dimethyl-L-lysine9
-
 ?
2.1.1.368 additional information H3K9 methylation by SETDB1 occurs in a distributive manner Homo sapiens ?
-
 ?
2.1.1.368 S-adenosyl-L-methionine + [histone H3 peptide 1-15]-L-lysine9
-
 Homo sapiens S-adenosyl-L-homocysteine + [histone H3 peptide 1-15]-N6-methyl-L-lysine9
-
 ?
2.1.1.368 S-adenosyl-L-methionine + [histone H3 peptide 1-15]-N6,N6-dimethyl-L-lysine9
-
 Homo sapiens S-adenosyl-L-homocysteine + [histone H3 peptide 1-15]-N6,N6,N6-trimethyl-L-lysine9
-
 ?
2.1.1.368 S-adenosyl-L-methionine + [histone H3 peptide 1-15]-N6-methyl-L-lysine9
-
 Homo sapiens S-adenosyl-L-homocysteine + [histone H3 peptide 1-15]-N6,N6-dimethyl-L-lysine9
-
 ?

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
2.1.1.366 0.005
-
 [histone H3 peptide 1-15]-N6,N6-dimethyl-L-lysine9 SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
2.1.1.366 0.013
-
 S-adenosyl-L-methionine substrate [histone H3 peptide 1-15]-N6,N6-dimethyl-L-lysine9, SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
2.1.1.366 0.038
-
 [histone H3 peptide 1-15]-N6,N6-dimethyl-L-lysine9 pH 7.6, 23°C Homo sapiens
2.1.1.366 0.065
-
 S-adenosyl-L-methionine substrate [histone H3 peptide 1-15]-N6,N6-dimethyl-L-lysine9, pH 7.6, 23°C Homo sapiens
2.1.1.368 0.027
-
 [histone H3 peptide 1-15]-L-lysine9 SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
2.1.1.368 0.045
-
 [histone H3 peptide 1-15]-N6-methyl-L-lysine9 SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
2.1.1.368 0.072
-
 S-adenosyl-L-methionine substrate [histone H3 peptide 1-15]-L-lysine9, SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
2.1.1.368 0.09
-
 S-adenosyl-L-methionine substrate [histone H3 peptide 1-15]-N6-methyl-L-lysine9, SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
2.1.1.368 0.192
-
 [histone H3 peptide 1-15]-L-lysine9 pH 7.6, 23°C Homo sapiens
2.1.1.368 0.293
-
 [histone H3 peptide 1-15]-N6-methyl-L-lysine9 pH 7.6, 23°C Homo sapiens
2.1.1.368 0.337
-
 S-adenosyl-L-methionine substrate [histone H3 peptide 1-15]-L-lysine9, pH 7.6, 23°C Homo sapiens
2.1.1.368 0.352
-
 S-adenosyl-L-methionine substrate [histone H3 peptide 1-15]-N6-methyl-L-lysine9, pH 7.6, 23°C Homo sapiens

kcat/KM [mM/s]

EC Number kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
2.1.1.366 0.013
-
 [histone H3 peptide 1-15]-N6,N6-dimethyl-L-lysine9 SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
2.1.1.366 0.026
-
 S-adenosyl-L-methionine substrate [histone H3 peptide 1-15]-N6,N6-dimethyl-L-lysine9, SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
2.1.1.366 0.089
-
 [histone H3 peptide 1-15]-N6,N6-dimethyl-L-lysine9 pH 7.6, 23°C Homo sapiens
2.1.1.366 0.098
-
 S-adenosyl-L-methionine substrate [histone H3 peptide 1-15]-N6,N6-dimethyl-L-lysine9, pH 7.6, 23°C Homo sapiens
2.1.1.368 0.095
-
 [histone H3 peptide 1-15]-L-lysine9 SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
2.1.1.368 0.11
-
 [histone H3 peptide 1-15]-N6-methyl-L-lysine9 SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
2.1.1.368 0.135
-
 S-adenosyl-L-methionine substrate [histoneH3 peptide 1-15]-L-lysine9, SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
2.1.1.368 0.167
-
 S-adenosyl-L-methionine substrate [histoneH3 peptide 1-15]-N6-methyl-L-lysine9, SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
2.1.1.368 0.467
-
 [histone H3 peptide 1-15]-L-lysine9 pH 7.6, 23°C Homo sapiens
2.1.1.368 0.495
-
 S-adenosyl-L-methionine substrate [histoneH3 peptide 1-15]-L-lysine9, pH 7.6, 23°C Homo sapiens
2.1.1.368 0.497
-
 [histone H3 peptide 1-15]-N6-methyl-L-lysine9 pH 7.6, 23°C Homo sapiens
2.1.1.368 0.628
-
 S-adenosyl-L-methionine substrate [histoneH3 peptide 1-15]-N6-methyl-L-lysine9, pH 7.6, 23°C Homo sapiens