Apabetalone

Apabetalone (RVX-208) is an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. The IC50s are 87 μM and 0.51 μM for BD1 and BD2, respectively[1].

Product Specifications

CAS Number

[1044870-39-4]

Product Name Alternative

RVX-208; RVX000222

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Epigenetic Reader Domain; HIV

Type

Reference compound

Related Pathways

Anti-infection; Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/RVX-208.html

Purity

99.34

Solubility

DMSO : ≥ 33 mg/mL

Smiles

COC1=CC(OC)=C(C(NC(C2=CC(C)=C(OCCO)C(C)=C2)=N3)=O)C3=C1

Molecular Formula

C20H22N2O5

Molecular Weight

370.40

Precautions

H302, H315, H319, H335

References & Citations

[1]Picaud S, et al. RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Proc Natl Acad Sci U S A. 2013 Dec 3;110 (49) :19754-9.|[2]McLure KG, et al. RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist. PLoS One. 2013 Dec 31;8 (12) :e83190.|[3]Jahagirdar R, et al. A novel BET bromodomain inhibitor, RVX-208, shows reduction of atherosclerosis in hyperlipidemic ApoE deficient mice. Atherosclerosis. 2014 Sep;236 (1) :91-100.