Table 2 ΔTm shifts (°C) of biotinylated BSP (BSP-a and BSP-b) tested against a panel of BET and other diverse BRDs.

Compounds (final concentration, 10 μM) were added to the proteins (final concentration, 2 μM); the temperature was increased from 25° to 96°C at a step of 3°C/min; excitation and emission filters for the SYPRO Orange dye were set to 465 and 590 nm; and experiments were performed in triplicate. Values are means ± SD.

ProteinΔTmobs (°C)
BSP-aBSP-b
BRD2(1)−7.5 ± 0.71.9 ± 0.5
BRD2(2)−0.4 ± 0.23.0 ± 0.2
BRD3(1)−2.7 ± 0.22.3 ± 0.3
BRD3(2)−3.0 ± 0.13.1 ± 0.0
BRD4(1)−2.7 ± 0.23.8 ± 0.3
BRD4(2)−5.1 ± 0.01.8 ± 0.3
BRDT(1)−5.0 ± 0.11.3 ± 0.3
BRDT(2)0.5 ± 0.10.9 ± 0.4
CECR24.3 ± 0.07.4 ± 0.1
CREBBP−3.1 ± 0.60.1 ± 0.4
TAF1(2)−12.4 ± 0.11.9 ± 0.1
TAF1L(2)0.2 ± 0.12.9 ± 0.4