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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Deubiquitinase (DUB)-BAY-805
BAY-805

Chemical Structure : BAY-805

CAS No.: 2925481-88-3

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BAY-805 (BAY805)

货号: 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.

规格 价格 库存 数量
5 mg ￥1380 In stock
10 mg ￥2180 In stock
25 mg ￥3780 In stock
50 mg ￥5880 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 507.58
分子式 C24H28F3N5O2S
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-[(1R)-1-[[5-[(4-Cyanophenyl)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl]-3-methyl-butyl]-1-(trifluoromethyl)cyclohexanecarboxamide

参考文献

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

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