AR-42

SKU: orb1222983

Description

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.

Key Properties

• CAS Number: 935881-37-1
• MW: 312.36
• Purity: >98% (HPLC)
• Formula: C₁₈H₂₀N₂O₃
• SMILES: CC(C)[C@H](C(=O)Nc1ccc(cc1)C(=O)NO)c1ccccc1
• Target: GluR
• Solubility: In Vitro: Ethanol : 50 mg/mL (160.07 mM)

Bioactivity

• In Vivo:
  Animal model: Nude mice (HepG2 cell tumor xenograft model). Dosage: 10 mg/kg. Administration: Tail vein injection; twice a week for three weeks. Result: Significantly inhibited tumor growth.
• In Vitro:
  Cell Proliferation Assay Cell line: Mouse (P815) and canine (C2 and BR) malignant mast cells. Concentration: 0.0625, 0.125, 0.25, 0.5, 1 μM Incubation time: 24 hours. Result: 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

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

Quick Database Links

Gene Symbol

GluR