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说明： RNF114 inhibitor
化学名： (2aR,5aR,6S,6aR,8R,9aR,10aS,10bR,10cR)-8-(3-Furanyl)-2a,5a,6,6a,8,9,9a,10a,10b,10c-decahydro-2a,5a,6a,7-tetramethyl-2,5-dioxo-2H,5H-cyclopenta[d']naphtho[1,8-bc:2,3-b']difuran-6-acetic acid methyl ester
纯度： ≥97% (HPLC)
生物活性 for Nimbolide
Nimbolide inhibits auto-ubiquitination of the E3 ligase RNF114 and p21 ubiquitination in vitro. This compound impairs proliferation of triple-negative breast cancer cell lines. Nimbolide also induces apoptotic cell death in a Waldenströms macroglobulinemia cell line (BCWM1) and inhibits tumor growth in a xenograft model of Waldenströms macroglobulinemia.
Nimbolide can be used for the development of Degraders that utilize RNF114 as an E3 ligase for Targeted Protein Degradation.
技术数据 for Nimbolide
| 分子量 | 466.53 |
| 公式 | C27H30O7 |
| 储存 | Store at -20°C |
| 纯度 | ≥97% (HPLC) |
| CAS Number | 25990-37-8 |
| PubChem ID | 12313376 |
| InChI Key | JZIQWNPPBKFOPT-LSYMHUITSA-N |
| Smiles | [H][C@@]12C[C@@H](C3=COC=C3)C(C)=C1[C@]4([C@@H]([C@]5(C(C=C[C@]6(C(O[C@@]([C@]4(O2)[H])([C@]56[H])[H])=O)C)=O)C)CC(OC)=O)C |
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 Nimbolide
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 46.65 | 100 |
制备储备液 for Nimbolide
以下数据基于产品分子量 466.53。 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 | 2.14 mL | 10.72 mL | 21.43 mL |
| 5 mM | 0.43 mL | 2.14 mL | 4.29 mL |
| 10 mM | 0.21 mL | 1.07 mL | 2.14 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.43 mL |
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产品说明书 for Nimbolide
参考文献 for Nimbolide
参考文献是支持产品生物活性的出版物。
Chitta et al (2014) Nimbolide targets BCL2 and induces apoptosis in preclinical models of Waldenströms macroglobulinemia. Blood Cancer J. 4 260 PMID: 25382610
Spradin et al (2019) Harnessing the anti-cancer natural product nimbolide for targeted protein degradation. Nat.Chem.Biol. 15 747 PMID: 31209351
Tong et al (2020) A nimbolide-based kinase degrader preferentially degrades oncogenic BCR-ABL. ACS Chem.Biol. 15 1788 PMID: 32568522
If you know of a relevant reference for Nimbolide, please let us know.
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关键词: Nimbolide, Nimbolide supplier, e3, ligase, RNF114, inhibitors, inhibits, ligands, targeted, protein, degradation, Ubiquitin, E3, Ligases, 7289, 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
This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:
- Active Degraders
- TAG Degradation Platform
- Degrader Building Blocks
- Assays for Protein Degradation
- Induced Proximity Tools
Programmed Cell Death Poster
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