935881-37-1
Chemical Structure
AR-42
Synonym(s): HDAC-42; OSU-HDAC42
- CAS No.: 935881-37-1
- Formula:C18H20N2O3
- Molecular Weight:312.36
IUPAC Name: (S)-N-hydroxy-4-(3-methyl-2-phenylbutanamido)benzamide
InChIKey: LAMIXXKAWNLXOC-INIZCTEOSA-N
SMILES: CC([C@@H](C1=CC=CC=C1)C(NC2=CC=C(C=C2)C(NO)=O)=O)C
Biological Activity: 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].
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AR-42 | 98.52% | 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. | ||||||||||||||||||||
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- [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. [Content Brief]
- [2]. Lu Q, et al. Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors. J Med Chem. 2005 Aug 25;48(17):5530-5. [Content Brief]
Keywords
