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BAY-805

Chemical Structure : BAY-805

CAS No.: 2925481-88-3

BAY-805 (BAY805)

Catalog No.: PC-49862Not For Human Use, Lab Use Only.

BAY-805 (BAY805) is the first highly potent, selective and non-covalent USP21 inhibitor with IC50 of 6 nM and 2 nM in HTRF and Ub-rhodamine biochemical assays (hUSP21), respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

BAY-805 (BAY805) is the first highly potent, selective and non-covalent USP21 inhibitor with IC50 of 6 nM and 2 nM in HTRF and Ub-rhodamine biochemical assays (hUSP21), respectively.
Cellular inhibition of USP21 with BAY-805 induced cellular NF-κB activation with an EC50 of 17 nM in the NF-κB reporter assays.
BAY-805 shows the strong competition effect and effectively prevents ubiquitin binding.
BAY-805 exhibites strong ligand-induced protein stabilization resulting in a substantial thermal shift in the melt curve of USP21.
BAY-805 exhibits no antiproliferative effect was observed in Jurkat, Molm-13, A549, MDA-MB-231, and U2OS cell lines at 30 uM.
BAY-805 shows no significant effect on the activity of any of other deubiquitinating enzyme (DUBs) target.

Physicochemical Properties

M.Wt 507.58
Formula C24H28F3N5O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-[(1R)-1-[[5-[(4-Cyanophenyl)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl]-3-methyl-butyl]-1-(trifluoromethyl)cyclohexanecarboxamide

References

1. Fabian Göricke, et al. J Med Chem. 2023 Feb 20. doi: 10.1021/acs.jmedchem.2c01933.

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