DN02 is a potent, selective BRD8 bromodomain probe. DN02 has exhibits high affinity for the BRD8(1) (Ki=32 nM), which is 30-fold more affinity than BRD8 (2) (Ki＞1000 nM)[1].
DN02 has (1 nM-100 μM) low nM AlphaScreen with IC50 value of 48 nM, with high selectivity over BRD9 and BRD4 in biochemical AlphaScreen assays[1].
DN02 (32 nM) has minimal off-target engagement across the bromodomain family, with modest activity against CBP/P300[1].
[1]. Remillard D, et, al. Chemoproteomics Enabled Discovery of Selective Probes for NuA4 Factor BRD8. ACS Chem Biol. 2021 Nov 19;16(11):2185-2192.