Bromodomain (BET) inhibitor. SARS-CoV-2 transmembrane protein E binds to the bromodomain-containing proteins BRD2 and BRD4. Gordon et al. bioRxiv, Mar 23 2020, https://doi.org/10.1101/2020.03.22.002386.
- Datasheet: view or download
- Applications:In clinical trials for other indication(s)
Biochemicals & reagents
1) Picaud et al. (2013), RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain; Proc. Natl. Acad. Sci. USA, 110 19754 2) McLure et al. (2013), RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist; PLoS One, 8 e83190 3) Bailey et al. (2010), RVX-208: a small molecule that increases apolipoprotein A-I and high-density lipoprotein cholesterol in vitro and in vivo; J. Am. Coll. Cardiol., 55 2580 4) Jahagirdar et al. (2014), A novel BET bromodomain inhibitor, RVX-208 shows reduction of atherosclerosis in hyperlipidemic ApoE deficient mice; Atherosclerosis, 236 91
RVX-208 is a potent BET bromodomain antagonist with IC50 of 0.510 μM for BD2, with approximately 170-fold selectivity over BD1 (1,2). This compound increases apolipoprotein A-1 and HDL cholesterol in vitro and in vivo (3) and reduces atherosclerosis (4).