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Potent and high affinity BRD inhibitor (IC50 = 32.5 - 42.5 nM; Kd = 50.5 - 61.3 nM). Inhibits myeloma cell proliferation. Attenuates transcription of oncogenic MYC and suppresses key inflammatory genes. Exhibits efficacy in a range of oncology and immunoinflammatory models. Displays antiproliferative effect in vitro and in vivo. Orally bioavailable.
|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|
Preparing Stock Solutions
The following data is based on the product molecular weight 423.9. 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||2.36 mL||11.8 mL||23.59 mL|
|5 mM||0.47 mL||2.36 mL||4.72 mL|
|10 mM||0.24 mL||1.18 mL||2.36 mL|
|50 mM||0.05 mL||0.24 mL||0.47 mL|
References are publications that support the biological activity of the product.
Chaidos et al (2014) Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762. Blood 123 697 PMID: 24335499
Mirguet et al (2013) Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains. J.Med.Chem. 56 7501 PMID: 24015967
Nicodeme et al (2010) Suppression of inflammation by a synthetic histone mimic. Nature 468 1119 PMID: 21068722
If you know of a relevant reference for I-BET 762, please let us know.
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Keywords: I-BET 762, I-BET 762 supplier, I-BET762, Potent, high, affinity, BRD, inhibitors, bromodomains, anti-inflammatory, orally, bioavailable, GSK525762A, Molibresib, Bromodomains, 6521, Tocris Bioscience
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
Epigenetics Research Bulletin
Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:
- DNA Methyltransferases
- Histone Deacetylases
- Histone Demethylases
- Histone Methyltransferases
Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.