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Biological Activity for BAY 299
BAY 299 is a potent and selective BRD1 and TAF1 inhibitor (IC50 values are 6-67 and 8-13 nM, respectively). Displays selectivity over other bromodomains (>30-fold over other members of the BRPF family; BRD9 and ATAD2; >300-fold over BRD4). Displays BRD1 and TAF1 inhibition in a NanoBRET cell assay. Inhibits binding of BRD1 and TAF1 to histone H4 (IC50 values are 575 nM and 0.9 μM, respectively) and histone H3.3 (IC50 values are 825 nM and 1.4 μM, respectively).
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the BAY 299 probe summary on the SGC website.
External Portal Information for BAY 299
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of BAY 299 is reviewed on the Chemical Probes website.
Compound Libraries for BAY 299
Technical Data for BAY 299
|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 BAY 299
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for BAY 299
The following data is based on the product molecular weight 429.47. 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||2.33 mL||11.64 mL||23.28 mL|
|5 mM||0.47 mL||2.33 mL||4.66 mL|
|10 mM||0.23 mL||1.16 mL||2.33 mL|
|50 mM||0.05 mL||0.23 mL||0.47 mL|
References for BAY 299
References are publications that support the biological activity of the product.
Klein et al (2014) Crosstalk between epigenetic readers regulates the MOZ/MORF HAT complexes. Epigenetics 9 186 PMID: 24169304
Bouche et al (2017) Benzoisoquinolinediones as potent and selective inhibitors of BRPF2 and TAF1/TAF1L bromodomains. J.Med.Chem. 60 4002 PMID: 28402630
If you know of a relevant reference for BAY 299, please let us know.
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Citations for BAY 299
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 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.