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76889
RVX-208
Activators & Inhibitors
Chemical Modulators

RVX-208 #76889

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Chemical structure of 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.

Product Description

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.

Background

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).

  1. Picaud, S. et al. (2013) Proc Natl Acad Sci U S A 110, 19754-9.
  2. McLure, K.G. et al. (2013) PLoS One 8, e83190.
  3. Bailey, D. et al. (2010) J Am Coll Cardiol 55, 2580-9.
  4. Tsujikawa, L.M. et al. (2019) Clin Epigenetics 11, 102.
  5. Wang, J. et al. (2020) PLoS Pathog 16, e1008429.
For Research Use Only. Not For Use In Diagnostic Procedures.

Cell Signaling Technology is a trademark of Cell Signaling Technology, Inc.

To Purchase # 76889S
Product # Size Price
76889S
10 mg N/A

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