Suprastat

Chemical Structure : Suprastat

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货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	386.452
分子式	C20H26N4O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 Month
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	4-((3-(4-(aminomethyl)phenyl)-1-(4-hydroxybutyl)ureido)methyl)-N-hydroxybenzamide

参考文献

1. Satish Noonepalle, et al. J Med Chem. 2020 Sep 24;63(18):10246-10262.

Suprastat

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Suprastat

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