AR-42

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 Specifications

CAS Number

[935881-37-1]

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.