CBK006377 | UPS inhibitor | Probechem Biochemicals

Chemical Structure : CBK006377

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CBK006377 (CBK77)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	333.318
分子式	C14H11N3O5S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(6-ethoxybenzo[d]thiazol-2-yl)-5-nitrofuran-2-carboxamide

参考文献

1. Tatiana A Giovannucci, et al. Cell Death Dis. 2021 Oct 6;12(10):914.

CBK006377 (CBK77)

生物&药学活性

物理化学性质&存储条件

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CBK006377 (CBK77)

生物&药学活性

物理化学性质&存储条件

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