RGNCY-0085 (9c HDAC6 degrader)
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).
Tags: Cancer, small molecule, HDAC, HDACs, RGNCY-0085, 9c, HDAC6, degrader