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Literature summary for 2.1.1.355 extracted from

  • Chang, Y.; Zhang, X.; Horton, J.R.; Upadhyay, A.K.; Spannhoff, A.; Liu, J.; Snyder, J.P.; Bedford, M.T.; Cheng, X.
    Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294 (2009), Nat. Struct. Mol. Biol., 16, 312-317.
    View publication on PubMed
Search for more literature for 2.1.1.355

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli BL21(DE3) cells Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with BIX-01294, hanging drop vapor diffusion method, using 0.1 M HEPES pH 7.5, 18-20% (w/v) polyethylene glycol 4000 and 7-10% (v/v) isopropanol, in the absence or presence of DMSO (6-36% v/v) Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
BIX-01294
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
nickel-chelating column chromatography, HiTrap-Q column chromatography, and Superdex-75 and -200 gel filtration Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
S-adenosyl-L-methionine + DNA methyltransferase 1
-
 Homo sapiens ?
-
 ?
S-adenosyl-L-methionine + histone H3(K9)
-
 Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
G9a
-
 Homo sapiens
G9a-like protein lysine methyltransferase
-
 Homo sapiens
GLP
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0007
-
 G9a-like protein lysine methyltransferase, in 20 mM Tris (pH 8.5), at 30°C Homo sapiens BIX-01294
0.0019
-
 histone lysine methyltransferase G9a, in 20 mM Tris (pH 8.5), at 30°C Homo sapiens BIX-01294