RGNCY-0085 (9c HDAC6 degrader)
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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).
Systematic Name: (E)-8-(2-(4-(2-(2-(2-(4-(((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)methyl)-1H-1,2,3-triazol-1-yl)ethoxy)ethoxy)ethoxy)benzylidene)hydrazinyl)-N-hydroxy-8-oxooctanamide
SMILES: ONC(CCCCCCC(N/N=C/C1=CC=C(OCCOCCOCCN2N=
NC(CNC3=CC=CC(C(N4C5C(NC(CC5)=O)=O)=O)=C3C4=O)=C2)C=C1)=O)=O
Formula: C37H45N9O10
Mol Wt: 775.33
PMID: 29871848
Tags: Cancer, small molecule, HDAC, HDACs, RGNCY-0085, 9c, HDAC6, degrader