Description | A BD2 bromodomain inhibitor; inhibits BD2 in BRD2, BRD3, and BRD4 (IC50s = 0.08, 0.05, and 0.02 µM, respectively) and is selective for BD2 over BD1 (IC50s = 3.76, 2.34, and 1.16 µM for BRD2, BRD3, and BRD4, respectively), as well as CREBBP and p300 (IC50s = >50 µM for both); decreases levels of the mRNAs encoding IL-6 and VCAM-1 in primary synovial fibroblasts isolated from patients with rheumatoid arthritis at 10 and 30 µM; It prevents LPS-induced increases in IL-6 and Ifn-γ serum levels in a mouse model of LPS-induced endotoxemia at 75 mg/kg; inhibits collagen-induced increases in ankle and knee diameter, cartilage damage, the ankle tissue levels of mRNAs encoding IL-1β, Mmp-3, Mmp-13, and Rankl, and ankle joint protein levels of IL-6 and VCAM-1 in a rat model of collagen-induced rheumatoid arthritis at 25, 50, and 75 mg/kg twice per day; improves gait and mobility and reverses body weight loss, as well as decreases the number of spinal cord inflammatory foci and apoptotic cells and reduces spinal nerve demyelination in a mouse model of EAE at 75 and 125 mg/kg per day |