PROTAC comprising BET antagonist (+)-JQ1 (Cat.No. 4499) conjugated to a cereblon E3 ubiquitin ligase ligand. Depletes BET bromodomains in cancer cell lines in vitro (EC50 = 430 nM in breast cancer cells) and induces apoptosis. Delays tumor growth and downregulates MYC in mice bearing human AML xenografts.
Sold under license from Dana-Farber Cancer Institute.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 785.27. Batch specific molecular weights may vary from batch to batch due to solvent 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||1.27 mL||6.37 mL||12.73 mL|
|5 mM||0.25 mL||1.27 mL||2.55 mL|
|10 mM||0.13 mL||0.64 mL||1.27 mL|
|50 mM||0.03 mL||0.13 mL||0.25 mL|
References are publications that support the products' biological activity.
Winter et al (2015) Drug Development. Phthalimide conjugation as a strategy for in vivo target protein degradation. Science 348 1376 PMID: 25999370
Wurz et al (2017) A "click chemistry platform" for the rapid synthesis of bispecific molecules for inducing protein degradation. J.Med.Chem. 10.1021 PMID: 28378579
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Keywords: dBET1, supplier, Proteolysis, Targeting, Chimera, PROTAC, cereblon, E3, ubiquitin, ligase, bromodomain, BRD4, degradation, Ubiquitin, E3, Ligases, PROTACs, Bromodomains, Ubiquitin, E3, Ligases, Tocris Bioscience
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