AR-42

Research use only, not for human use.

AR-42 is an HDAC inhibitor (IC50: 30 nM).

AR-42, also known as (S)-HDAC-42; AR-42; NSC-736012; OSU-42; OSU-HDAC-42; OSUHDAC-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.

Cell Proliferation Assay Cell Line:Mouse (P815) and canine (C2 and BR) malignant mast cellsConcentration:0.0625, 0.125, 0.25, 0.5, 1 μMIncubation Time:24 hoursResult:Inhibited cell proliferation in a dose-dependent manner, and the median IC50s for P815, C2, and BR cells were 0.65, 0.30, and 0.23 μM, respectively. Cell Cycle Analysis Cell Line:P815,C2 cells Concentration:0.5 μM Incubation Time:24 hours Result:Induced cell-cycle arrest at G1 in the P815 cells and at G1/G2 in the C2 cells.Apoptosis Analysis Cell Line:P815, C2, BR cells Concentration:0.13, 0.25, 0.5, 1 μM Incubation Time:24 hours Result:Caused a dose-dependent induction of apoptosis.Western Blot Analysis Cell Line:P815, C2, BR cell lines Concentration:0.5, 1, 3 μM Incubation Time:24 hours Result:A dose-dependent hyperacetylation of histone H3, histone H4, and α-tubulin.

Animal Model:Nude mice (HepG2 cell tumor xenograft model) Dosage:10 mg/kg Administration:Tail vein injection; twice a week for three weeksResult:Significantly inhibited tumor growth.

AR42 | AR 42 | (S)-HDAC-42 | AR-42 | NSC-736012 | OSU-42

Neuroscience

GluR

HDAC

Cancer

——

935881-37-1

312.36

C18H20N2O3

>98% (HPLC)

In Vitro:?Ethanol : 50 mg/mL (160.07 mM)

CC(C)[C@H](C(=O)Nc1ccc(cc1)C(=O)NO)c1ccccc1

(S)-N-hydroxy-4-(3-methyl-2-phenylbutanamido)benzamide

(-20℃)

With Ice Pack

≥ 2 years