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Chemical Structure : CBK006377
Catalog No.: PC-72569Not For Human Use, Lab Use Only.
CBK006377 (CBK77) is a small molecule inhibitor of the ubiquitin-proteasome system (UPS) with EC50 of 4.3 uM in MelJuSo Ub-YFP cells (6h treatment).
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CBK006377 (CBK77) is a small molecule inhibitor of the ubiquitin-proteasome system (UPS) with EC50 of 4.3 uM in MelJuSo Ub-YFP cells (6h treatment).
CBK77 (16h treatment, 10 uM) causes an irreversible, global impairment of the UPS collapse, accompanied by a general accumulation of ubiquitylated proteins and caspase-dependent cell death.
CBK77 causes a global impairment of ubiquitin-dependent proteasomal degradation without global inhibition of proteasome or DUB activity.
NAD(P)H:quinone oxidoreductase 1 (NQO1) is a critical factor for CBK77-mediated UPS impairment, CBK77 is an NQO1 substrate, efficiently metabolized by NQO1.
CBK77 reduces growth of NQO1-proficient human cancer cells and xenograft tumors in mice without overt signs of toxicity.
| M.Wt | 333.318 | |
| Formula | C14H11N3O5S | |
| Appearance | Solid | |
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1. Tatiana A Giovannucci, et al. Cell Death Dis. 2021 Oct 6;12(10):914.
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