AR-42

• Description :

  AR-42 (HDAC-42; OSU-HDAC42) is a potent, orally bioavailable pan-HDAC inhibitor (IC50=16 nM) . AR-42 induces growth inhibition, cell-cycle arrest, apoptosis, and activation of caspases-3/7. AR-42 promotes hyperacetylation of H3, H4, and alpha-tubulin, and up-regulation of p21. AR-42 shows cytotoxicity against various human cancer cell lines[1][2].

• Product Name Alternative :

  HDAC-42; OSU-HDAC42

• UNSPSC :

  12352005

• Hazard Statement :

  H302, H315, H319, H335

• Target :

  Apoptosis; Autophagy; HDAC

• Type :

  Reference compound

• Related Pathways :

  Apoptosis; Autophagy; Cell Cycle/DNA Damage; Epigenetics

• Applications :

  Cancer-programmed cell death

• Field of Research :

  Cancer

• Assay Protocol :

  https://www.medchemexpress.com/ar-42.html

• Purity :

  98.52

• Solubility :

  DMSO : 10 mg/mL (ultrasonic) |Ethanol : 50 mg/mL (ultrasonic)

• Smiles :

  CC([C@@H](C1=CC=CC=C1)C(NC2=CC=C(C=C2)C(NO)=O)=O)C

• Molecular Formula :

  C18H20N2O3

• Molecular Weight :

  312.36

• Precautions :

  H302, H315, H319, H335

• References & Citations :

  [1]Lu YS, Chou CH, Tzen KY, Gao M, ChLu YS, et al. Radiosensitizing effect of a phenylbutyrate-derived histone deacetylase inhibitor in hepatocellular carcinoma. Int J Radiat Oncol Biol Phys. 2012 Jun 1;83 (2) :e181-9.eng AL, Kulp SK, Cheng JC.Radiosensitizing effect of a phenylbutyrate-derived histone deacetylase inhibitor in hepatocellular carcinoma.Int J Radiat Oncol Biol Phys. 2012 Jun 1;83 (2) :e181-9. Epub 2012 Feb 28.|[2]Lu Q, et al. Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors. J Med Chem. 2005 Aug 25;48 (17) :5530-5.|[3]Lin TY, et al. AR-42, a novel HDAC inhibitor, exhibits biologic activity against malignant mast cell lines via down-regulation of constitutively activated Kit. Blood. 2010 May 27;115 (21) :4217-25.|[4]Zhang M, et al. AR-42 induces apoptosis in human hepatocellular carcinoma cells via HDAC5 inhibition. Oncotarget. 2016 Apr 19;7 (16) :22285-94.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 1

• CAS Number :

  [935881-37-1]