AR-42

  • Chemical Properties
CAS No. 935881-37-1 Cat. No. BCP26343
Name AR-42
Synonyms REC-2282;REC2282;REC 2282;(S)-HDAC-42; NSC-736012; OSU-HDAC42;HDAC-42;HDAC 42;HDAC42;AR 42;AR42; OSUHDAC-42;
Formula C18H20N2O3 M. Wt 312.36
  • Biological Activity
Description AR-42 , a derivative of hydroxamate-tethered phenylbutyrate, is a novel and potent inhibitor of histone deacetylase (HDAC) that potently inhibits the activity of HDAC with 50% inhibition concentration IC50 value of 16 nM and induces histone H3 acetylation, α-tubulin acetylation and p21 up-regulation, which have been considered as the hallmark indicators of HDAC inhibition. AR-42 has been found to modulate several apoptosis inhibitors as well as cell survival regulator, including Akt, Bcl-xL, Bax, Ku70 and surviving, and exert potent antitumor activity against multiple tumor types, such as human prostate and hepatic cancers, at least partially through PI3K/Akt pathway inhibition.AR-42 is a broad-spectrum deacetylase inhibitor of both histone and non-histone proteins, which has demonstrated greater potency and activity in solid tumors and hematological malignancies when compared in preclinical studies to vorinostat (also known as "SAHA" or Zolinza®), the first of two marketed compound in the class. AR-42 may possess additional histone-independent mechanisms, which may contribute to its superior profile in vitro and in vivo.
Pathways Cell Cycle/DNA Damage Epigenetics 
Targets HDAC 

Structure

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