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ChemicalBook > Product Catalogue >Biochemical Engineering >Inhibitors >Epigenetics >Epigenetic Reader Domain inhibitors >RVX-208

RVX-208

RVX-208 Structure
  • ₹0
  • Product name: RVX-208
  • CAS: 1044870-39-4
  • MF: C20H22N2O5
  • MW: 370.4
  • EINECS:
  • MDL Number:MFCD18633270
  • Synonyms:2-(4-(2-hydroxyethoxy)-3,5-diMethylphenyl)-5,7-diMethoxyquinazolin-4(3H)-one;RVX-000222;4(3H)-Quinazolinone, 2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-;2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-4(3H)-quinazolinone RVX-208;RVX-208;Apabetalone;Apabetalone-RVX-208;RVX-208(RVX 000222)
Manufacturer Product number Product description Packaging Price Updated Buy

Properties

Boiling point :594.2±60.0 °C(Predicted)
Density :1.28±0.1 g/cm3(Predicted)
storage temp. :-20°C (des.)
solubility :Soluble in DMSO (up to 75 mg/ml) or in Ethanol (up to 4 mg/ml).
form :solid
pka :14.21±0.10(Predicted)
color :White
Stability :Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.

Safety Information

Symbol(GHS): GHS hazard pictograms
Signal word: Warning
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H371 May cause damage to organs Specific target organ toxicity, single exposure Category 2 Warning P260, P264, P270, P309+P311, P405,P501
Precautionary statements:
P260 Do not breathe dust/fume/gas/mist/vapours/spray.
P264 Wash hands thoroughly after handling.
P264 Wash skin thouroughly after handling.
P270 Do not eat, drink or smoke when using this product.
P309+P311 IF exposed or if you feel unwell: call a POISON CENTER or doctor/physician.
P405 Store locked up.
P501 Dispose of contents/container to..…

Description

The bromodomain and extra terminal (BET) proteins interact with acetylated lysine-containing sequences on target proteins via their bromodomains, commonly altering gene transcription. The human BET proteins contain two bromodomains, the first (BD1) being closer to the N-terminus than the second (BD2). RVX-208 is a selective antagonist of BET bromodomains, binding with 10-100-fold higher affinity for BD2 (IC50 = 0.04-0.28 μM) over BD1 (IC50 = 1.8-3.1 μM). RVX-208 causes the selective release of BET proteins from chromatin in cells. It interferes with the BET protein BRD4, resulting in an increased expression of apolipoprotein (Apo) A1 in cells, mice, monkeys, and humans. RVX-208 also reduces atherosclerosis in hyperlipidemic ApoE-deficient mice.

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