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WS 383 is a potent and reversible DCN1-UBC12 interaction inhibitor (IC50 = 11 nM). The compound displays selectivity for DCN1-UBC12 over inhibition of a panel of kinases. including Bruton's tyrosine kinase (BTK), cyclin-dependent kinases (CDKs) and epidermal growth factor receptor (EGFR). In vitro, WS 383 selectively inhibits cullin-3 neddylation over other cullins, and induces accumulation of p21, p27 and NRF2.
WS 383 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
|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 498.45. 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||2.01 mL||10.03 mL||20.06 mL|
|5 mM||0.4 mL||2.01 mL||4.01 mL|
|10 mM||0.2 mL||1 mL||2.01 mL|
|50 mM||0.04 mL||0.2 mL||0.4 mL|
References are publications that support the biological activity of the product.
Wang et al (2019) Development of highly potent, selective, and cellular active triazolo[1,5- a]pyrimidine-based inhibitors targeting the DCN1-UBC12 protein-protein interaction. J.Med.Chem. 62 2772 PMID: 30803229
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Keywords: WS 383, WS 383 supplier, WS383, ubiquitin, E3, E2, ligase, interaction, inhibitor, inhibits, protein-protein, Cul3/1, neddylation, CRL, cullin-RING, ligases, Ubiquitin, Ligases, Ubiquitin/Ubl, Conjugating, Enzymes, 7055, Tocris Bioscience
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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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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