Synonyms: BAY 86-5274 | MS-275 | SNDX-275 | ZK 244894
Compound class:
Synthetic organic
Comment: Entinostat (MS-275) inhibits Class I histone deacetylases (HDACs 1, 2, 3 & 8), but has been shown to be somewhat selective for HDAC1 [1,4]. Studies in rodent models of inflammation suggest that inhibition by entinostat may be clinically useful [2,6-8], perhaps more so than broader acting Class I HDAC inhibitors such as vorinostat (SAHA) [6].
![]() Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
1. Bradner JE, West N, Grachan ML, Greenberg EF, Haggarty SJ, Warnow T, Mazitschek R. (2010)
Chemical phylogenetics of histone deacetylases. Nat Chem Biol, 6 (3): 238-243. [PMID:20139990] |
2. Cantley MD, Bartold PM, Marino V, Fairlie DP, Le GT, Lucke AJ, Haynes DR. (2011)
Histone deacetylase inhibitors and periodontal bone loss. J Periodont Res, 46 (6): 697-703. [PMID:21745207] |
3. Dear AE. (2016)
Epigenetic Modulators and the New Immunotherapies. N Engl J Med, 374 (7): 684-6. [PMID:26886527] |
4. Hu E, Dul E, Sung CM, Chen Z, Kirkpatrick R, Zhang GF, Johanson K, Liu R, Lago A, Hofmann G et al.. (2003)
Identification of novel isoform-selective inhibitors within class I histone deacetylases. J Pharmacol Exp Ther, 307 (2): 720-8. [PMID:12975486] |
5. Khan N, Jeffers M, Kumar S, Hackett C, Boldog F, Khramtsov N, Qian X, Mills E, Berghs SC, Carey N et al.. (2008)
Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors. Biochem J, 409 (2): 581-9. [PMID:17868033] |
6. Lin HS, Hu CY, Chan HY, Liew YY, Huang HP, Lepescheux L, Bastianelli E, Baron R, Rawadi G, Clément-Lacroix P. (2007)
Anti-rheumatic activities of histone deacetylase (HDAC) inhibitors in vivo in collagen-induced arthritis in rodents. Br J Pharmacol, 150 (7): 862-72. [PMID:17325656] |
7. Zhang ZY, Schluesener HJ. (2012)
HDAC inhibitor MS-275 attenuates the inflammatory reaction in rat experimental autoimmune prostatitis. Prostate, 72 (1): 90-9. [PMID:21538420] |
8. Zhang ZY, Zhang Z, Schluesener HJ. (2010)
MS-275, an histone deacetylase inhibitor, reduces the inflammatory reaction in rat experimental autoimmune neuritis. Neuroscience, 169 (1): 370-7. [PMID:20451583] |