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RVX 208
- RVX 000222 - Apabetalone
- Soluble in DMSO
- MF: C20H22N2O5
- MW: 370.4
Description
RVX 208 (Apabetalone) is a BET bromodomain inhibitor with preference for second bromodomains (BD2), including BRD3 BD2, where AlphaScreen data report markedly greater activity than at BRD3 BD1. It binds the acetyl-lysine pocket competitively and has been associated with increased apolipoprotein A-I (ApoA1) expression.
BET proteins regulate transcriptional programs involved in inflammation, lipid metabolism and cardiovascular disease. RVX 208 is useful for studying BD2-selective bromodomain pharmacology, ApoA1 regulation and epigenetic modulation of cardiometabolic pathways.
Key Features
- BD2-preferring BET bromodomain inhibitor
- Selectivity over BD1 within BET family members
- Peptide-competitive acetyl-lysine pocket binding
- Modulates ApoA1-related transcriptional programs
Applications
- BET bromodomain pharmacology
- ApoA1 and HDL biology studies
- Cardiometabolic epigenetics research
- Inflammation and transcriptional regulation assays
More Information
| Parent CAS No. | 1044870-39-4 |
|---|---|
| Chemical Name | 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one |
| SMILES | N1C2=C(C(OC)=CC(OC)=C2)C(=O)NC=1C1=CC(C)=C(OCCO)C(C)=C1 |
| MFCD | MFCD18633270 |
| InChi | InChI=1S/C20H22N2O5/c1-11-7-13(8-12(2)18(11)27-6-5-23)19-21-15-9-14(25-3)10-16(26-4)17(15)20(24)22-19/h7-10,23H,5-6H2,1-4H3,(H,21,22,24) |
| InChiKey | NETXMUIMUZJUTB-UHFFFAOYSA-N |
| CID | 135564749 |
| Short Description | BET inhibitor |
References
- S. Picaud et al. RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Proc. Natl. Acad. Sci. U.S.A. 2013, 110, 19754-19759.
- K.G. McLure et al. RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist. PLoS One. 2013, 8, e83190.
- E. McNeill, Eileen. RVX-208, a stimulator of apolipoprotein AI gene expression for the treatment of cardiovascular diseases. Curr. Opini. Invest. Drugs. 2010, 11, 357-364.
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