AR-42

AR‑42 is a small molecule, orally available, broad-spectrum histone deacetylase inhibitor (HDACi), structurally related to phenylbutyrate. It inhibits both histone and non-histone protein deacetylation with high potency against class I and II HDACs. Mechanistically, AR‑42 induces hyperacetylation of histones H3/H4 and α-tubulin, upregulates p21WAF/CIP1 expression, inhibits the gp130/STAT3 pathway as well as PI3K/Akt signaling, leading to cell cycle arrest and apoptosis in various tumor cells including multiple myeloma, lymphoma, prostate cancer, ovarian cancer, meningioma and schwannoma. The drug has demonstrated greater potency than vorinostat in preclinical models. It has been designated an orphan drug by the FDA for meningioma and schwannoma of the central nervous system[1][2][4][5].

Other names

N-hydroxy-4-[[(2S)-3-methyl-2-phenylbutanoyl]amino]benzamide(S)-(+)-N-hydroxy-4-(3-methyl–2–phenyl-butyrylamino)–benzamide(αS)-N-[4–[(Hydroxyamino)carbonyl]phenyl]-α-(1-methylethyl)benzeneacetamideBENZENEACETAMIDE, N-(4–((HYDROXYAMINO)CARBONYL)PHENYL)-.ALPHA.-(1-METHYLETHYL)-, (.ALPHA.S)