DC_G16-11 GCN5 inhibitor RGNCY-0086
Per 10 mg
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
Mol Wt: 655.06
Xiong, H. et al. Discovery of 1,8-acridinedione derivatives as novel GCN5 inhibitors via high throughput screening. European Journal of Medicinal Chemistry 151 (2018) 740e751.
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