Nimbolide

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Cat.No. 7289 - Nimbolide | C27H30O7 | CAS No. 25990-37-8
Description: RNF114 inhibitor
Chemical Name: (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
Purity: ≥97% (HPLC)
Datasheet
Citations
Reviews
Literature (3)

Biological Activity 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.

Technical Data for Nimbolide

M. Wt 466.53
Formula C27H30O7
Storage Store at -20°C
Purity ≥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

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.

Solubility Data for Nimbolide

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 46.65 100

Preparing Stock Solutions for Nimbolide

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.

Select a batch to recalculate based on the batch molecular weight:
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

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References for Nimbolide

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


If you know of a relevant reference for Nimbolide, please let us know.

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Keywords: Nimbolide, Nimbolide supplier, e3, ligase, RNF114, inhibitors, inhibits, ligands, targeted, protein, degradation, Ubiquitin, E3, Ligases, 7289, Tocris Bioscience

Citations for Nimbolide

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Literature in this Area

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Targeted Protein Degradation

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

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

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