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Synonyms: compound 7b [PMID: 31414801] | SS208
Compound class: Synthetic organic
Comment: SS-208 is reported as an isotype selective inhibitor of histone deacetylase 6 (HDAC6) . It has been developed for potential to treat advanced melanoma. SS-208 has been designed to provide improved HDAC6 selectivity compared to ricolinostat and citarinostat which both exhibit unfavourable levels of HDAC1 inhibition.
Selective pharmacological inhibition or genetic abrogation of HDAC6 modulates immune checkpoint activity by downregulating the expression of PD-L1 via the recruitment and activation of STAT3 . The antitumour activity of SS-208 in vivo is primarily mediated by activation of immune cells and an anti-tumour immune response in the tumour microenvironment.
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. M L, P PV, T K, M P, E S, J P, K V W, C L, F C, S D et al.. (2016)
Essential role of HDAC6 in the regulation of PD-L1 in melanoma.
Mol Oncol, 10 (5): 735-750. [PMID:26775640]
2. Shen S, Hadley M, Ustinova K, Pavlicek J, Knox T, Noonepalle S, Tavares MT, Zimprich CA, Zhang G, Robers MB et al.. (2019)
Discovery of a New Isoxazole-3-hydroxamate-Based Histone Deacetylase 6 Inhibitor SS-208 with Antitumor Activity in Syngeneic Melanoma Mouse Models.
J Med Chem, 62 (18): 8557-8577. [PMID:31414801]