Evotec Munich
Evotec Munich
Evotec Munich
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0,01<br />
0,1<br />
1<br />
10<br />
K d [µM]<br />
PAGE 7<br />
UNC0638 BIX-01294<br />
N<br />
O<br />
O<br />
N<br />
WIZ<br />
GLP<br />
G9a<br />
Protein X<br />
OCR<br />
NH<br />
N<br />
N<br />
Cellular Target Profiling <br />
Profiling of methyltransferase inhibitors<br />
N<br />
H<br />
N<br />
WIZ<br />
GLP<br />
G9A<br />
N N<br />
N<br />
O<br />
O<br />
Cellular target proteins for the published G9a selective<br />
methyltransferase inhibitors UNC0638 and BIX-01294 were<br />
identified in human CML (K562) cells<br />
Comparison with published in vitro data revealed known as well<br />
as previously unknown target proteins for both compounds<br />
Protein UNC0638<br />
K dµM<br />
<strong>Evotec</strong><br />
UNC0638<br />
IC 50µM<br />
Vedadi et al<br />
BIX-01294<br />
K dµM<br />
<strong>Evotec</strong><br />
BIX-01294<br />
IC 50µM<br />
Vedadi et al<br />
WIZ 0,039 - 0,056 -<br />
GLP 0,099 0,019 0,101 0,034<br />
Protein X 0,270 - -<br />
G9A 0,152 < 0,015 0,294 0,180<br />
OCR 4,524 - - -<br />
WIZ Widely-interspaced zinc finger-containing protein, mediating EHMT1 / EHMT2 interaction<br />
Protein X Possible UNC0638 off-target protein, validation experiments ongoing<br />
OCR Spindlin-1 / Ovarian cancer-related protein<br />
Vedadi et al, 2007, Nat Chem Biol., 7:566-74
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