29
SGC‐CBP30: A Chemical Probe for CBP/p300 Bromodomains
Bromodomains (BRDs)
Binding – ITC
Selectivity (ΔTm)
Time (min)
0
30
60
90
µcal/sec
0.00
-0.20
-0.40
-6.00
-1
kcal mol of injectant
0.00
-3.00
-9.00
-12.00
0.0
0.5
1.0
1.5
2.0
2.5
Molar Ratio
O
Fragment to probe
SGC‐CBP30
N
N
H3C
N
O
CH3
N
O
CH3
Cl
CH3
•
•
•
•
•
CBP Kd = 21 nM (ITC).
Selective over other BRD families.
40‐fold selectivity over BRD4 (ITC).
Active in cells (μM).
Available to order from SGC.
SGC‐CBP30
Cellular characterisation
FRAP
Crystalography
FRET
Control
p53 reporter assay
SGC‐CBP30
1.
Duncan A. Hay1,2, Paul E. Brennan2, Stuart Conway1, Oleg Fedorov2, Panagis Filippakopoulos2, Stefan Knapp2, Susanne MullerKnapp2, Sarah Martin2, Martin Philpott2, Sarah Picaud2, Chris Schofield1, Tony Tumber2, Chris Wells2, Clarence Yapp2.
2.