Evotec Munich

0,1
1
10
K d M
PAGE 14
K d [µM]
MIER3
C16orf87
SIN3A
SIN3B
MIER1
NCOR1
RCOR2
NCOR2
MIER2
CHD3
GPS2
BHC80
ZNF217
GSE1
BRAF35
CoREST
HDAC1
RERE
ZNF261
AOF2
GATAD2A
RCOR3
HDAC2
IRA1
WDR5
MTA3
TBL1
GATAD2B
CHD4
MTA1
MBD3
RBBP4
HMG20A
HDAC3
MTA2
ISOC2
ZNF198
RBBP7
HDAC6
DBP5
MBD2
KPNA3
PP3476
HDAC10
KPNA4
LAMB2
ALDH2
MBLAC2
CK2a1
ALDH1B1
TTC38
HDAC8
Epigenetics Target Profiling
Profiling of SAHA (Vorinostat) using a generic matrix
80
80
60
60
40
40
HDAC1 20
20
0,19
120
100
100
80
80
60
60
40
HDAC4 40
-
20
20
% Bound
0
-20
120
20
0
-20
1
10 102
Conc [µM]
120
120
100
100
80
80
60
60
40
HDAC5 40
-
20
20
100
100
80
80
60
60
HDAC7 -
40
40
% Bound
% Bound
0
-20
120
20
0
-20
1
10 102
Conc [µM]
120
100
100
80
80
60
60
HDAC6 40
0,43
40
1
10 102
Conc [µM]
120
100
100
80
80
60
60
HDAC8 6,5
40
40
% Bound
120
20
0
-20
1
10 102
Conc [µM]
100
100
80
80
60
60
HDAC10 0,79
40
40
% Bound
% Bound
% Bound
120
100
0
-20
120
100
0
-20
120
20
0
-20
1
10 102
Conc [µM]
80
80
60
60
40
40
HDAC2 0,24
20
20
% Bound
120
100
0
-20
1
10 102
Conc [µM]
80
80
60
60
40
40
HDAC3 0,35
20
20
HDAC
Known HDAC complex partner
Other proteins
Target profile in human ovarian cancer (A2780) cells
% Bound
Binding Competition K d M
1
10 102
Conc [µM]
1
10 102
Conc [µM]
1
10 102
Conc [µM]
% Bound
% Bound
% Bound
% Bound
% Bound
% Bound
% Bound
% Bound
% Bound
120
100
0
-20
120
100
0
-20
120
100
0
-20
120
0
-20
0
-20
20
0
-20
120
20
0
-20
20
0
-20
120
20
0
-20
-2
10 10-1 100 101
Conc [µM]
-2
10 10-1 100 101
Conc [µM]
-2
10 10-1 100 101
Conc [µM]
-2
10 10-1 100 101
Conc [µM]
-2
10 10-1 100 101
Conc [µM]
-2
10 10-1
Conc [µM]
100 101
-2
10 10-1 100 101
Conc [µM]
-2
10 10-1 100 101
Conc [µM]
-2
10 10-1 100 101
Conc [µM]
Epigenetics Target Profiling allows for
maximum HDAC coverage and constitutes
a native assay under conditions that
preserve the integrity of HDAC complexes