| Chemical Properties | Back Directory | [density ]
1.31±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
Solid | [pka]
8.17±0.50(predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
BAY-805 is a selective inhibitor of ubiquitin-specific protease USP21. BAY-805 has high selectivity for deubiquitinating enzyme (DUB) targets, kinases, proteases and other common target enzymes[1]. | [Biological Activity]
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 assay2 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) th at effectively upregulates cellular NF-KB 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). | [References]
[1] G?ricke F, et al. Discovery and Characterization of BAY-805, a Potent and Selective Inhibitor of Ubiquitin-Specific Protease USP21. J Med Chem. 2023 Feb 20. DOI:10.1021/acs.jmedchem.2c01933 |
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| Company Name: |
Merck KGaA
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| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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