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
Keywords: OXF BD 02, supplier, OXFBD02, selective, bromodomains, BRD, BRD4(1), inhibitors, cell, permeable, antiproliferative, inhibits, Bromodomains, Bromodomains, Tocris Bioscience
