Product 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.
Molecular Weight | 370.4 g/mol |
Purity | >98% |
Molecular Formula | C20H22N2O5 |
CAS | 1044870-39-4 |
Solubility | Soluble in DMSO at 75 mg/ml or ethanol at 4 mg/ml. |
RVX-208 is a potent and selective inhibitor of bromodomain and extra terminal (BET) proteins, with a much stronger affinity for BD2 (IC50 = 0.510 μM) over BD1 (IC50 = 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 in vitro and in vivo, making BRD4 disruptors important compounds to study in relation to viral diseases (5).
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Cat. # | Size | Qty. | Price |
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76889S | 10 mg |
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