Martinostat Explained

Iupac Name:	(2E)-3-(4-phenyl)-N-hydroxyacrylamide
Cas Number:	1629052-58-9
Unii:	8JJC99KHGL
Chemspiderid:	34987952
C:	22
H:	30
N:	2
O:	2
Smiles:	CN(Cc1ccc(cc1)/C=C/C(=O)NO)CC23CC4CC(C2)CC(C4)C3

Martinostat is a histone deacetylase inhibitor (HDACi) that is potent against recombinant class I HDACs (isoforms 1-3) and class IIb HDAC (isoform 6) with low nanomolar affinities.^[1] In tissue CETSA assays,^[2] martinostat exhibits selectivity for class I HDACs (isoforms 1-3).^[3] When tagged with the radioisotope carbon-11, martinostat can be used to quantify HDAC in the brain and peripheral organs using positron emission tomography. Martinostat was given a name that adopted the style of other HDAC inhibitors, such as vorinostat, entinostat, and crebinostat, that recognized the academic center in which it was developed, the Martinos Center for Biomedical Imaging.

Notes and References

1. Wang C, Schroeder FA, Wey HY, Borra R, Wagner FF, Reis S, Kim SW, Holson EB, Haggarty SJ, Hooker JM . 6 . In vivo imaging of histone deacetylases (HDACs) in the central nervous system and major peripheral organs . EN . Journal of Medicinal Chemistry . 57 . 19 . 7999–8009 . October 2014 . 25203558 . 4191584 . 10.1021/jm500872p .
2. Jafari R, Almqvist H, Axelsson H, Ignatushchenko M, Lundbäck T, Nordlund P, Martinez Molina D . 14939791 . The cellular thermal shift assay for evaluating drug target interactions in cells . Nature Protocols . 9 . 9 . 2100–22 . September 2014 . 25101824 . 10.1038/nprot.2014.138 .
3. Wey HY, Gilbert TM, Zürcher NR, She A, Bhanot A, Taillon BD, Schroeder FA, Wang C, Haggarty SJ, Hooker JM . 6 . Insights into neuroepigenetics through human histone deacetylase PET imaging . Science Translational Medicine . 8 . 351 . 351ra106 . August 2016 . 27510902 . 5784409 . 10.1126/scitranslmed.aaf7551 .