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Chemical Structure : Suprastat
Catalog No.: PC-72090Not For Human Use, Lab Use Only.
Suprastat is a novel potent, selective inhibitor of histone deacetylase 6 (HDAC6) with IC50 of 0.9 nM.
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Suprastat is a novel potent, selective inhibitor of histone deacetylase 6 (HDAC6) with IC50 of 0.9 nM.
Suprastat did not show activity against the class IV isoform HDAC11 up to 50 uM, >290-fold selectivity over class I isoform HDAC1−HDAC3 and HDAC8 and 1000-fold selectivity over class IIa isoform HDAC4, HDAC5, HDAC7, and HDAC9.
Suprastat increased the levels of acetylated α-tubulin (Ac-α-tubulin) in WM164 human
melanoma cell line at 0.1-10 uM, the increase in Ac-α-tubulin was also associated with a slight increase in the levels of acetylated histone H3 (Ac-H3).
Suprastat mediated immunomodulatory effects by affecting HDAC6 interaction with the STAT3 transcription factor, decreased expression of IL10 gene, dose-dependent increase in the levels of Ac-α-tubulin in compound treated RAW 264.7 macrophages, decreased Y705 phosphorylation of STAT3.
A combination of Suprastat and anti-PD1 immunotherapy enhances antitumor immune response, mediated by a decrease of protumoral M2 macrophages and increased infiltration of antitumor CD8+ effector and memory T-cells.
| M.Wt | 386.452 | |
| Formula | C20H26N4O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Satish Noonepalle, et al. J Med Chem. 2020 Sep 24;63(18):10246-10262.
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