CST, 76889S, RVX-208

Product Usage Information
RVX-208 is supplied as a lyophilized powder. For a 20 mM stock, reconstitute 10 mg of powder in 1.35 ml of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.
Storage
Store lyophilized at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.
Background
RVX-208 is a potent and selective inhibitor of bromodomain and extra terminal (BET) proteins, with a much stronger affinity for BD2 (IC = 0.510 μM) over BD1 (IC = 87 μM) (1,2). BET proteins interact with acetylated lysine-containing sequences to transcriptionally regulate several cellular processes. BRD4, a BET protein that mediates induction of Apolipoprotein A-I (ApoA-I) mRNA, can be disrupted at the binding site by RVX-208. This leads to altered transcription, resulting in increased ApoA-I production and high-density lipoprotein cholesterol (HDL-C) levels, both of which are promising in the treatment of atherosclerosis and vascular inflammation (2-4). Recently, BRD4 inhibition has shown anti-viral activity and increased host resistance to several DNA and RNA viruses and , making BRD4 disruptors important compounds to study in relation to viral diseases (5).
Alternate Names
2-[4-2-hydroxyethoxy-35-dimethylphenyl]-57-dimethoxy-43H-quinazolinone