产品说明
一般描述
A cell-permeable bis-nitrobenzylidene-piperidinone that inhibits 19S deubiquitinase (DUB) activity (IC50 = 2.1 µM against Ub-AMC hydrolysis) in a reversible manner by directly targeting UCH37/UCH-L5 and USP14, while exhibiting little or no activity toward BAP1, UCH-L1, UCH-L3, USP2, USP7, USP8 (IC50 >100 µM), or POH1/PRN11. Dual UCH37 and USP14 inhibition by a-AP15 results in increased bulk cellular protein ubiquitination level and a blockage of protein proteasomal degradation (Effective conc. ≥770 nM in HCT-116 cells), exactly opposite to the effects seen with USP14 inhibition alone by IU1 (Cat. No. 662210). Effectively suppresses the growth of various tumors in mice (2.5 to 5 mg/kg, i.p. or s.c.) in vivo.
包装
10 mg in Glass bottle
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
D′Arcy, P., et al. 2011. Nat. Med.17, 1636.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
| 经验(实验)分子式 | C22H17N3O6 |
| 分子量 | 419.39 |
| MDL编号 | MFCD26142662 |
产品性质
| 质量水平 | 100 |
| 测定 | ≥97% (HPLC) |
| 形式 | powder |
| manufacturer/tradename | Calbiochem® |
| 储存条件 | OK to freeze protect from light |
| 颜色 | yellow |
| 溶解性 | DMSO: 100 mg/mL, clear, yellow |
| 运输 | ambient |
| 储存温度 | 2-8℃ |
| SMILES string | O=C(/C(CN(C(C=C)=O)C/1)=C/C(C=C2)=CC=C2[N+]([O-])=O)C1=C\C3=CC=C(C=C3)[N+]([O-])=O |
安全信息
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 3 |
