Martinostat

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.

11C-labeled martinostat
Martinostat
Identifiers
  • (2E)-3-(4-{[(Adamantan-1-ylmethyl)(methyl)amino]methyl}phenyl)-N-hydroxyacrylamide
CAS Number
ChemSpider
UNII
Chemical and physical data
FormulaC22H30N2O2
Molar mass354.494 g·mol−1
3D model (JSmol)
  • CN(Cc1ccc(cc1)/C=C/C(=O)NO)CC23CC4CC(C2)CC(C4)C3

References
  1. Wang C, Schroeder FA, Wey HY, Borra R, Wagner FF, Reis S, et al. (October 2014). "In vivo imaging of histone deacetylases (HDACs) in the central nervous system and major peripheral organs". Journal of Medicinal Chemistry. 57 (19): 7999–8009. doi:10.1021/jm500872p. PMC 4191584. PMID 25203558.
  2. Jafari R, Almqvist H, Axelsson H, Ignatushchenko M, Lundbäck T, Nordlund P, Martinez Molina D (September 2014). "The cellular thermal shift assay for evaluating drug target interactions in cells". Nature Protocols. 9 (9): 2100–22. doi:10.1038/nprot.2014.138. PMID 25101824. S2CID 14939791.
  3. Wey HY, Gilbert TM, Zürcher NR, She A, Bhanot A, Taillon BD, et al. (August 2016). "Insights into neuroepigenetics through human histone deacetylase PET imaging". Science Translational Medicine. 8 (351): 351ra106. doi:10.1126/scitranslmed.aaf7551. PMC 5784409. PMID 27510902.
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