Synonyms: CI-994 | CI994
Compound class:
Synthetic organic
Comment: Tacedinaline inhibits the histone deacetylase enzyme HDAC1 [6], and is reported to have antitumour activity in preclinical studies [2,4-5].
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. Gediya LK, Belosay A, Khandelwal A, Purushottamachar P, Njar VC. (2008)
Improved synthesis of histone deacetylase inhibitors (HDIs) (MS-275 and CI-994) and inhibitory effects of HDIs alone or in combination with RAMBAs or retinoids on growth of human LNCaP prostate cancer cells and tumor xenografts. Bioorg Med Chem, 16 (6): 3352-60. [PMID:18166465] |
3. Liu L, Chen B, Qin S, Li S, He X, Qiu S, Zhao W, Zhao H. (2010)
A novel histone deacetylase inhibitor Chidamide induces apoptosis of human colon cancer cells. Biochem Biophys Res Commun, 392 (2): 190-5. [PMID:20060381] |
4. Loprevite M, Tiseo M, Grossi F, Scolaro T, Semino C, Pandolfi A, Favoni R, Ardizzoni A. (2005)
In vitro study of CI-994, a histone deacetylase inhibitor, in non-small cell lung cancer cell lines. Oncol Res, 15 (1): 39-48. [PMID:15839304] |
5. LoRusso PM, Demchik L, Foster B, Knight J, Bissery MC, Polin LM, Leopold 3rd WR, Corbett TH. (1996)
Preclinical antitumor activity of CI-994. Invest New Drugs, 14 (4): 349-56. [PMID:9157069] |
6. Methot JL, Chakravarty PK, Chenard M, Close J, Cruz JC, Dahlberg WK, Fleming J, Hamblett CL, Hamill JE, Harrington P et al.. (2008)
Exploration of the internal cavity of histone deacetylase (HDAC) with selective HDAC1/HDAC2 inhibitors (SHI-1:2). Bioorg Med Chem Lett, 18 (3): 973-8. [PMID:18182289] |