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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.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 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.
|Concentration / Solvent Volume / Mass||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|
References are publications that support the biological activity of the product.
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
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Keywords: Nimbolide, Nimbolide supplier, e3, ligase, RNF114, inhibitors, inhibits, ligands, targeted, protein, degradation, Ubiquitin, E3, Ligases, 7289, Tocris Bioscience
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Targeted Protein Degradation Research Product Guide
This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:
- Active Degraders
- Degrader Building Blocks
- Custom Degrader Services
- UPS Proteins and Assays
- Assays for Protein Degradation
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