9H-Indeno[1,2-b]pyrazine-2,3-dicarbonitrile, 9-[(phenylmethoxy)imino]-

DUB-IN-1 is an active inhibitor of ubiquitin-specific proteases (USPs), with an IC50 of 0.85 μM for USP8[1].

Potent and selective ubiquitin specific peptidase USP8 deubiquitinase (DUB) inhibitor.

DUB-IN-1 is a potent and selective ubiquitin specific peptidase USP8 deubiquitinase (DUB) inhibitor (IC50 = 850 nM/USP8, >100 μM/USP7). DUB-IN-1 inhibits the proliferation (200-800 nM for 24 or 48h; LN229, U87MG, and T98G cells), invasion (500-800 nM for 48 or 96h; LN229 and T98G cells), and stemness (500-800 nM for 7 or 14 days; LN229 and T98G cells) in GBM cultures.

[1] Colombo M, et al. Synthesis and biological evaluation of 9-oxo-9H-indeno[1,2-b]pyrazine-2,3-dicarbonitrile analogues as potential inhibitors of deubiquitinating enzymes. ChemMedChem. 2010 Apr 6;5(4):552-8. DOI:10.1002/cmdc.200900409