BAY 299

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Cat.No. 5970 - BAY 299 | C25H23N3O4 | CAS No. 2080306-23-4
Description: Potent and selective BRD1 and TAF1 inhibitor
Chemical Name: 6-(3-Hydroxypropyl)-2-(1,3,6-trimethyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-yl)-1H-benzo[de]isoquinoline-1,3(2H)-dione
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Potent and selective BRD1 and TAF1 inhibitor (IC50 values are 6-67 and 8-13 nM, respectively). Displays selectivity over other bromodomains (>30-fold over other members of the BRPF family; BRD9 and ATAD2; >300-fold over BRD4). Displays BRD1 and TAF1 inhibition in a NanoBRET cell assay. Inhibits binding of BRD1 and TAF1 to histone H4 (IC50 values are 575 nM and 0.9 μM, respectively) and histone H3.3 (IC50 values are 825 nM and 1.4 μM, respectively).

Licensing Information

This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the BAY 299 probe summary on the SGC website.

Technical Data

M. Wt 429.47
Formula C25H23N3O4
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2080306-23-4
PubChem ID 122705990
InChI Key OFWWWKWUCDUISA-UHFFFAOYSA-N
Smiles OCCCC1=CC=C(C(N2C3=C(C)C=C(N(C)C(N4C)=O)C4=C3)=O)C5=C1C=CC=C5C2=O

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 42.95 100

Preparing Stock Solutions

The following data is based on the product molecular weight 429.47. 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 2.33 mL 11.64 mL 23.28 mL
5 mM 0.47 mL 2.33 mL 4.66 mL
10 mM 0.23 mL 1.16 mL 2.33 mL
50 mM 0.05 mL 0.23 mL 0.47 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Klein et al (2014) Crosstalk between epigenetic readers regulates the MOZ/MORF HAT complexes. Epigenetics 9 186 PMID: 24169304

Bouche et al (2017) Benzoisoquinolinediones as potent and selective inhibitors of BRPF2 and TAF1/TAF1L bromodomains. J.Med.Chem. 60 4002 PMID: 28402630


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Keywords: BAY299 potent BRD1 TAF1 inhibitors inhibits bromodomains and PHD Finger Transcription initiation factor TFIID subunits 1 Bromodomains

Citations for BAY 299

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Literature in this Area

Cancer

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
  • Angiogenesis
  • Invasion and Metastasis
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.

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