BET bromodomain inhibitor specific for second bromodomains (BD2s), currently in phase I/II clinical trials for the treatment of cardiovascular diseases (IC50 values of 87 and 0.51 μM derived from the AlphaScreen data on BRD3 BD1 and BD2 resp.). RVX 208 preferentially binds to the second bromodomain found on BET proteins, exhibiting selectivity over BD1 of up to 23-fold with a KD of 195 nM against BD2 and 4 μM against BD1 of BRD3. RVX 208 binds to the acetyl-lysine binding pocket in a peptide-competitive manner, and leads to an increase of plasma levels of the high-density lipid protein ApoA1, wich has emerged as a promising approach for the treatment of atherosclerosis.