OXF BD 02
Biological Activity
Selective inhibitor of the first bromodomain of BRD4 (BRD4(1)) (IC50 = 382 nM). Exhibits 2-3-fold selectivity for BRD4(1) over the CBP bromodomain and has little affinity for a range of other bromodomains. Reduces viability of lung adenocarcinoma cell lines and attenuates proliferation of MV-4-11 leukemia cells. Cell permeable.
Licensing Information
Sold with the agreement of the University of Oxford
Compound Libraries
OXF BD 02 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 295.33 |
| Formula | C18H17NO3 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1429129-68-9 |
| PubChem ID | 56929801 |
| InChI Key | FEQUIPXIENTMJN-UHFFFAOYSA-N |
| Smiles | OC1=CC(C2=C(C)ON=C2C)=CC(C(O)C3=CC=CC=C3)=C1 |
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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 29.53 | 100 | |
| ethanol | 2.95 | 10mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 295.33. 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 | 3.39 mL | 16.93 mL | 33.86 mL |
| 5 mM | 0.68 mL | 3.39 mL | 6.77 mL |
| 10 mM | 0.34 mL | 1.69 mL | 3.39 mL |
| 50 mM | 0.07 mL | 0.34 mL | 0.68 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Hewings et al (2011) 3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands. J.Med.Chem. 54 6761 PMID: 21851057
Hewings et al (2013) Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands. J.Med.Chem. 56 3217 PMID: 23517011
If you know of a relevant reference for OXF BD 02, please let us know.
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Keywords: OXF BD 02, supplier, OXFBD02, selective, bromodomains, BRD, BRD4(1), inhibitors, cell, permeable, antiproliferative, inhibits, Bromodomains, Bromodomains, Tocris Bioscience
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Cancer Research Product Guide
A collection of over 750 products for cancer research, the guide includes research tools for the study of:
- Cancer Metabolism
- Epigenetics in Cancer
- Receptor Signaling
- Cell Cycle and DNA Damage Repair
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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:
- Bromodomains
- DNA Methyltransferases
- Histone Deacetylases
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- 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.
