BAY 299

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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)
Literature (4)

Biological Activity for BAY 299

BAY 299 is a 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.

External Portal Information for BAY 299 is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of BAY 299 is reviewed on the Chemical Probes website.

Compound Libraries for BAY 299

BAY 299 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

Technical Data for BAY 299

M. Wt 429.47
Formula C25H23N3O4
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2080306-23-4
PubChem ID 122705990
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for BAY 299

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 42.95 100

Preparing Stock Solutions for BAY 299

The following data is based on the product molecular weight 429.47. 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.

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 for BAY 299

Certificate of Analysis / Product Datasheet
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References for BAY 299

References are publications that support the biological activity of the product.

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

If you know of a relevant reference for BAY 299, please let us know.

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Citations for BAY 299

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Literature in this Area

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