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Submit ReviewOXF BD 02
Description: Selective BRD4(1) inhibitor
Chemical Name: 3-(3,5-Dimethyl-4-isoxazolyl)-5-hydroxy-α-phenylbenzenemethanol
Purity: ≥98% (HPLC)
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
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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 29.53 | 100 | |
| ethanol | 2.95 | 10 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 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 | 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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References
References are publications that support the biological activity of the product.
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
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Keywords: OXF BD 02, OXF BD 02 supplier, OXFBD02, selective, bromodomains, BRD, BRD4(1), inhibitors, cell, permeable, antiproliferative, inhibits, Bromodomains, 4928, Tocris Bioscience
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