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Biological Activity for iBET-BD2
iBET-BD2 is a potent and selective pan-BD2 inhibitor (IC50 values are 49, 98, 214 and 264 nM for BRD4BD2, BRD3BD2, BRDTBD2 and BRD2BD2, respectively). iBET-BD2 is selective for BD2 over BD1 (IC50 values are 10965, 36317, 70558, and >50119 µM for BRD2BD1, BRD3BD1, BRD4BD1, and BRDTBD1, respectively) in a time-resolved FRET (TR-FRET) assay. iBET-BD2 (1 μM) inhibits IFN-γ-induced protein expression of MHC class I in K562 cells. iBET-BD2 reduces the production of anti-KLH IgM antibodies in mice immunized with keyhole limpet hemocyanin (KLH). iBET-BD2 exhibits immunomodulatory activity. iBET-BD2 is orally bioavailable.
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the iBET-BD2 probe summary on the SGC website.
Compound Libraries for iBET-BD2
Technical Data for iBET-BD2
|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 iBET-BD2
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for iBET-BD2
The following data is based on the product molecular weight 414.48. 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||2.41 mL||12.06 mL||24.13 mL|
|5 mM||0.48 mL||2.41 mL||4.83 mL|
|10 mM||0.24 mL||1.21 mL||2.41 mL|
|50 mM||0.05 mL||0.24 mL||0.48 mL|
References for iBET-BD2
References are publications that support the biological activity of the product.
Gilan et al (2020) Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation. Science 368 387 PMID: 32193360
Preston et al (2020) Design and synthesis of a highly selective and in vivo-capable inhibitor of the second bromodomain of the bromodomain and extra terminal domain family of proteins. J.Med.Chem. 63 9070 PMID: 32691591
If you know of a relevant reference for iBET-BD2, please let us know.
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Keywords: iBET-BD2, iBET-BD2 supplier, GSK046, GSK-046, GSK, 046, iBET, BD2, iBETBD2, pan-BD2, selective, inhibitors, inhibits, SGC, Bromodomains, 7458, Tocris Bioscience
Citations for iBET-BD2
Citations are publications that use Tocris products.
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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 in Cancer PosterUpdated
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.