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Submit ReviewJB 300 is a potent and selective Aurora A Degrader (PROTAC®; DC50 = 30 nM and Dmax = 78%). It comprises a cereblon E3-ligase ligand Thalidomide (Cat. No. 0652) joined by a PEG2 linker to the Aurora A inhibitor MK-5108. The compound depletes Aurora A in MV4-11 cell lines and exhibits no degradation of Aurora B at 10 µM. JB 300 shows dose-dependent cytotoxicity in AML cells.
Aurora A antibodies validated for Simple Western™ (automated Western) instruments and Western Blot also available: Catalog # AF3295 and NBP1-51843.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Sold under license from University of Würzburg
M. Wt | 906.38 |
Formula | C43H45ClFN7O10S |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 3038446-90-8 |
InChI Key | LAZHTWDJEQSMOY-NKEKBGIASA-N |
Smiles | O=C([C@@]1(CC2=CC=CC(NC3=NC=CS3)=N2)CC[C@H](OC4=C(F)C(Cl)=CC=C4)CC1)NCCOCCOCCNC(COC5=C6C(N(C7CCC(NC7=O)=O)C(C6=CC=C5)=O)=O)=O |
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 | |
---|---|---|---|
Solubility | |||
DMSO | 18.13 | 20 |
The following data is based on the product molecular weight 906.38. 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 |
---|---|---|---|
0.2 mM | 5.52 mL | 27.58 mL | 55.16 mL |
1 mM | 1.1 mL | 5.52 mL | 11.03 mL |
2 mM | 0.55 mL | 2.76 mL | 5.52 mL |
10 mM | 0.11 mL | 0.55 mL | 1.1 mL |
References are publications that support the biological activity of the product.
Adhikari et al (2020) PROTAC-mediated degradation reveals a non-catalytic function of AURORA-A kinase. Nat.Chem.Biol. 16 1179 PMID: 32989298
Bozolovic et al (2022) Novel, highly potent PROTACs targeting AURORA-A kinase. Curr.Res.Chem.Biol. 2 100032
If you know of a relevant reference for JB 300, please let us know.
Keywords: JB 300, JB 300 supplier, JB300, AURORA-A, PROTACs, Degraders, degrades, kinase., Aurora, Kinases, Kinase, 7837, 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 your Targeted Protein Degradation and Induced Proximity research, including:
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