RGNCY-0086 (DC_G16-11 GCN5 inhibitor )

DC_G16-11 is a novel highly potent inhibitor of GCN5 (general control nonrepressed protein 5) which plays a crucial role in many biological processes and its dysregulation is closely associated with cancers.  The binding between GCN5 and DC_G16-11 was demonstrated by NMR and SPR with a KD of 4.2 µM.  DC_G16-11 inhibits proliferation and induces cell cycle arrest and apoptosis in cancer cells (MV4-11) with minimal effects on normal cells (HUV-EC-C). DC_G16-11 has great potential for clinical disease treatment. IC50 = 6.8 µM.

Systematic Name: 4-((2,6-dibromo-4-(3,3,6,6-tetramethyl-1,8-dioxo-1,2,3,4,5,6,7,8,9,10-decahydroacridin-9-yl)phenoxy)methyl)benzoic acid

SMILES:  OC(C1=CC=C(COC2=C(Br)C=C(C3C(C(CC(C)(C)C4)=O)=C4NC(CC(C)(C)C5)=C3C5=O)C=C2Br)C=C1)=O

Formula: C31H31Br2NO5

Mol Wt:  655.06

PMID:  29665527