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生化/生理作用
Potent and selective dual USP21 deubiquitinase (DUB) inhibitor with anti-cancer efficacy.
BAY-805 is a higly potent and selective USP21 deubiquitinase (DUBs) inhibitor (IC50 (Emax) = 6 nM (95%) by HTRF assay, 2 nM (87%) by Ub-Rh110 assay; Kd = 2.2 nM by SPR-based competition assay; 50/53% inhibition of USP10/USP22 at 10 µM, <31% inhibition against other DUBs) that effectively upregulates cellular NF-κB activation (7-fold increase at 10 µM 20h post BAY-805 treatment by HEK293T-based reporter assay) with good target engagement (EC50 = 17 nM by USP21 HiBiT CESTA assay).
BAY-805 is a higly potent and selective USP21 deubiquitinase (DUBs) inhibitor (IC50 (Emax) = 6 nM (95%) by HTRF assay, 2 nM (87%) by Ub-Rh110 assay; Kd = 2.2 nM by SPR-based competition assay; 50/53% inhibition of USP10/USP22 at 10 µM, <31% inhibition against other DUBs) that effectively upregulates cellular NF-κB activation (7-fold increase at 10 µM 20h post BAY-805 treatment by HEK293T-based reporter assay) with good target engagement (EC50 = 17 nM by USP21 HiBiT CESTA assay).
储存分类代码
11 - Combustible Solids
WGK
WGK 3
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Not applicable
闪点(°C)
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分析证书(COA)
Lot/Batch Number
Fabian Göricke et al.
Journal of medicinal chemistry, 66(5), 3431-3447 (2023-02-22)
USP21 belongs to the ubiquitin-specific protease (USP) subfamily of deubiquitinating enzymes (DUBs). Due to its relevance in tumor development and growth, USP21 has been reported as a promising novel therapeutic target for cancer treatment. Herein, we present the discovery of
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