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说明： Covalent RNF114 ligand
化学名： 1-[3,5-bis(4-Bromophenyl)-4,5-dihydro-1H-pyrazol-1-yl]-2-chloroethanone
纯度： ≥98% (HPLC)
生物活性 for EN 219
EN 219 is a covalent RNF114 inhibitor (IC50 = 470 nM). In vitro EN 219 mimics the mechanism of action of Nimbolide (Cat. No. 7289) by binding to RNF114 and inhibiting ubiquitination of its endogenous substrate, the tumor suppressor p21.
技术数据 for EN 219
| 分子量 | 456.56 |
| 公式 | C17H13Br2ClN2O |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 380351-29-1 |
| PubChem ID | 3413196 |
| InChI Key | CXRHMHAKZPJNKS-UHFFFAOYSA-N |
| Smiles | ClCC(N1N=C(C2=CC=C(C=C2)Br)CC1C3=CC=C(C=C3)Br)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for EN 219
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 45.66 | 100 | |
| ethanol | 9.13 | 20 |
制备储备液 for EN 219
以下数据基于产品分子量 456.56。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.19 mL | 10.95 mL | 21.9 mL |
| 5 mM | 0.44 mL | 2.19 mL | 4.38 mL |
| 10 mM | 0.22 mL | 1.1 mL | 2.19 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
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产品说明书 for EN 219
参考文献 for EN 219
参考文献是支持产品生物活性的出版物。
Luo et al (2021) Chemoproteomics-enabled discovery of covalent RNF114-based degraders that mimic natural product function. Cell Chem.Biol. 28 559 PMID: 33513350
If you know of a relevant reference for EN 219, please let us know.
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关键词: EN 219, EN 219 supplier, EN219, ligase, RNF114, e3, inhibitors, inhibits, ligands, targeted, protein, TPD, Degrader, Degraders, Ubiquitin, E3, Ligases, 7476, Tocris Bioscience
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
TPD and Induced Proximity Research Product GuideUpdated
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- TAG Degradation Platform
- Degrader Building Blocks
- Assays for Protein Degradation
- Induced Proximity Tools
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There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.
Targeted Protein Degradation Poster
Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia