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.
Sold with the agreement of the University of Oxford
OXF BD 02 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 29.53 | 100 | |
ethanol | 2.95 | 10mM with gentle warming |
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 |
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
Tocris Bioscience是一家专卖生命科学研究chemicals, peptides and antibodies的知名品牌,其产品也广为各大药厂、大学、研究机构,超过五万名科学研究者所采用。 目前,產品內容已超過一千六百種以上,並每年持續不斷的增加新的產品。目前,产品内容已超过一千六百种以上,并每年持续不断的增加新的产品。
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