- Guide to PHARMACOLOGY
Compound class: Synthetic organic
Comment: Quisinostat is an HDAC inhibitor. The compound has highest potency for HDAC1 and modest potency with HDACs 2, 4, 10, and 11. Quisinostat exhibits >30-fold selectivity against HDACs 3, 5, 8, and 9, with lowest potency for HDACs 6 and 7 .
The compound also has antimalarial activity . The Malaria tab on this ligand page provides additional curator comments of relevance to the Guide to MALARIA PHARMACOLOGY.
Ligand Activity Visualisation Charts
These 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.✖
1. Arts J, King P, Mariën A, Floren W, Beliën A, Janssen L, Pilatte I, Roux B, Decrane L, Gilissen R et al.. (2009)
JNJ-26481585, a novel "second-generation" oral histone deacetylase inhibitor, shows broad-spectrum preclinical antitumoral activity.
Clin Cancer Res, 15 (22): 6841-51. [PMID:19861438]
2. Huang Z, Li R, Tang T, Ling D, Wang M, Xu D, Sun M, Zheng L, Zhu F, Min H et al.. (2020)
A novel multistage antiplasmodial inhibitor targeting Plasmodium falciparum histone deacetylase 1.
Cell Discov, 6 (1): 93. [PMID:33311461]
3. Stühmer T, Arts J, Chatterjee M, Borawski J, Wolff A, King P, Einsele H, Leo E, Bargou RC. (2010)
Preclinical anti-myeloma activity of the novel HDAC-inhibitor JNJ-26481585.
Br J Haematol, 149 (4): 529-36. [PMID:20331455]
4. Tong WG, Wei Y, Stevenson W, Kuang SQ, Fang Z, Zhang M, Arts J, Garcia-Manero G. (2010)
Preclinical antileukemia activity of JNJ-26481585, a potent second-generation histone deacetylase inhibitor.
Leuk Res, 34 (2): 221-8. [PMID:19682743]
5. Wang M, Tang T, Li R, Huang Z, Ling D, Zheng L, Ding Y, Liu T, Xu W, Zhu F et al.. (2022)
Drug Repurposing of Quisinostat to Discover Novel Plasmodium falciparum HDAC1 Inhibitors with Enhanced Triple-Stage Antimalarial Activity and Improved Safety.
J Med Chem, 65 (5): 4156-4181. [PMID:35175762]