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76889
RVX-208
Activators & Inhibitors
Chemical Modulators

RVX-208 #76889

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RVX-208: Image 1
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.

Limited Uses

Except as otherwise expressly agreed in a writing signed by a legally authorized representative of CST, the following terms apply to Products provided by CST, its affiliates or its distributors. Any Customer's terms and conditions that are in addition to, or different from, those contained herein, unless separately accepted in writing by a legally authorized representative of CST, are rejected and are of no force or effect.

Products are labeled with For Research Use Only or a similar labeling statement and have not been approved, cleared, or licensed by the FDA or other regulatory foreign or domestic entity, for any purpose. Customer shall not use any Product for any diagnostic or therapeutic purpose, or otherwise in any manner that conflicts with its labeling statement. Products sold or licensed by CST are provided for Customer as the end-user and solely for research and development uses. Any use of Product for diagnostic, prophylactic or therapeutic purposes, or any purchase of Product for resale (alone or as a component) or other commercial purpose, requires a separate license from CST. Customer shall (a) not sell, license, loan, donate or otherwise transfer or make available any Product to any third party, whether alone or in combination with other materials, or use the Products to manufacture any commercial products, (b) not copy, modify, reverse engineer, decompile, disassemble or otherwise attempt to discover the underlying structure or technology of the Products, or use the Products for the purpose of developing any products or services that would compete with CST products or services, (c) not alter or remove from the Products any trademarks, trade names, logos, patent or copyright notices or markings, (d) use the Products solely in accordance with CST Product Terms of Sale and any applicable documentation, and (e) comply with any license, terms of service or similar agreement with respect to any third party products or services used by Customer in connection with the Products.

For Research Use Only. Not For Use In Diagnostic Procedures.
Cell Signaling Technology is a trademark of Cell Signaling Technology, Inc.
To Purchase # 76889
Cat. # Size Qty. Price
76889S
10 mg
$ 138