OXF BD 02

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Cat.No. 4928 - OXF BD 02 | C18H17NO3 | CAS No. 1429129-68-9
Description: Selective BRD4(1) inhibitor
Chemical Name: 3-(3,5-Dimethyl-4-isoxazolyl)-5-hydroxy-α-phenylbenzenemethanol
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

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.

Select a batch to recalculate based on the batch molecular weight:
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

Safety Datasheet

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


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

Citations for OXF BD 02

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Literature in this Area

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Cancer Research Product Guide

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  • Cancer Metabolism
  • Epigenetics in Cancer
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Epigenetics

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

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
  • Histone Demethylases
  • Histone Methyltransferases
Cell Cycle & DNA Damage Repair

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.

Pathways for OXF BD 02

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