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Biological Activity for I-BET 762
I-BET 762 is a potent and high affinity BET bromodomain 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.
Technical Data for I-BET 762
|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.
Solubility Data for I-BET 762
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for I-BET 762
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 for I-BET 762
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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Citations for I-BET 762
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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* 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
Epigenetics in Cancer Poster
Adapted from the 2015 Cancer Product Guide Edition 3, this poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
Rheumatoid Arthritis Poster
Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.