9c HDAC6 degrader RGNCY-0085
Per 10 mg
Compound 9c is the first small molecule histone deacetylase 6 (HDAC6) degrader. Over-expression of HDACs have been observed in cancers and other diseases. 9c is a degrader of zinc-dependent HDACs. 9c degrades HDAC6 in a dose dependent manner in MCF-7 cells and results in a concomitant increase in alpha-tubulin which is expected with the degradation of HDAC6. Furthermore,mechanistic studies suggested that HDAC6 was selectively removed by the ubiquitin-proteasome-system (UPS).
Yang, K., et al. Development of the first small molecule histone deacetylase 6 (HDAC6) degraders. Bioorganic & Medicinal Chemistry Letters (2018), https://doi.org/10.1016/j.bmcl.2018.05.057.
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