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C25-140 binds directly to TNF receptor-associated factor 6 (TRAF6) and inhibits its interaction with ubiquitin-conjugating enzyme Ubc13. C25-140 reduces TRAF6-Ubc13 activity and decreases NF-κB activation and inflammatory signaling in vitro. C25-140 exhibits selectivity for TRAF6 over other E3 ligases except cIAP1. In in vivo mouse models of autoimmune psoriasis and rheumatoid arthritis, the compound improves disease symptoms. The compound also suppresses the pro-inflammatory signaling activity of IL-17A and prevents its inhibitory effect on the anti-HBV action of IFN-α HepG2 cells.
|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|
The following data is based on the product molecular weight 457.57. 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|
|0.5 mM||4.37 mL||21.85 mL||43.71 mL|
|2.5 mM||0.87 mL||4.37 mL||8.74 mL|
|5 mM||0.44 mL||2.19 mL||4.37 mL|
|25 mM||0.09 mL||0.44 mL||0.87 mL|
References are publications that support the biological activity of the product.
Brenke et al (2018) Targeting TRAF6 E3 ligase activity with a small-molecule inhibitor combats autoimmunity. J.Biol.Chem. 293 13191 PMID: 29950522
Zhang et al (2022) Interleukin-17A pretreatment attenuates the anti-hepatitis B virus efficacy of interferon-alpha by reducing activation of the interferon-stimulated gene factor 3 transcriptional complex in hepatitis B virus-expressing HepG2 cells. Virol.J. 19 28 PMID: 35144643
If you know of a relevant reference for C25-140, please let us know.
Keywords: C25-140, C25-140 supplier, inhibits, inhibitors, TRAF6-Ubc13, NF-kB, NF-KappaB, κ, E3, ligases, Ubiquitin, Ligases, NF-kB/IkB, 7715, Tocris Bioscience
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This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:
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.
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