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- HSP (Heat shock proteins)
- EN219
EN219
An RNF114 recruiter
此产品仅用于科学研究，我们不为任何个人用途提供产品和服务
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包装价格促销价数量
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1mg￥250.00200.00- +
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5mg￥1225.00980.00- +
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10mg￥2125.001700.00- +
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25mg￥4662.003730.00- +
- 货号: ajcx25226
- CAS: 380351-29-1
- 别名:
- 分子式: C17H13Br2ClN2O
- 分子量: 456.6
- 纯度: ＞98%
- 溶解度: DMF: 10 mg/ml,DMSO: 5 mg/ml,Ethanol: 1 mg/ml
- 储存: -20°C
- 库存: 现货
Background
EN219 is a synthetic recruiter of the E3 ubiquitin ligase RNF114.1 It binds to cysteine 8 (C8) in the intrinsically disordered region of RNF114 (RNF114-C8; IC50 = 470 nM) and inhibits RNF114-induced autoubiquitination and p21 ubiquitination in a cell-free assay when used at a concentration of 50 µM. EN219 (1 µM) also interacts with cysteine residues in the tubulin β1 chain (TUBB1), heat shock protein 60 (Hsp60), also known as Hsp family D member 1 (HspD1), and histone H3.1 (HIST1H3A) in 231MFP human breast cancer cells in a proteomic profiling assay. It has been linked to the bromodomain and extra terminal domain (BET) inhibitor ligand (+)-JQ1 for use as a proteolysis-targeting chimera (PROTAC) to degrade bromodomain-containing protein 4 (BRD4) in 231MFP cells.
1.Luo, M., Spradlin, J.N., Boike, L., et al.Chemoproteomics-enabled discovery of covalent RNF114-based degraders that mimic natural product functionCell Chem. Biol.28(4)559-566(2021)
