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Description: Potent BRD9/7 inhibitor
Chemical Name: 3-(6-Acetylpyrrolo[1,2-a]pyrimidin-8-yl)-N-cyclopropyl-4-methylbenzamide
Purity: ≥98% (HPLC)
Biological Activity
Potent BRD9/7 inhibitor (Kd values are 33 and 340 nM, respectively) Exhibits >30-fold selectivity for BRD9 over other bromodomains except BRD7. Cell permeable and active in vivo.
Negative Control also available.
Licensing Information
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the TP 472 probe summary on the SGC website.
Compound Libraries
TP 472 is also offered as part of the Tocriscreen Epigenetics Toolbox. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 333.38 |
| Formula | C20H19N3O2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| PubChem ID | 123773279 |
| InChI Key | RPBMXJHQYJLPDN-UHFFFAOYSA-N |
| Smiles | O=C(C)C1=CC(C2=CC(C(NC3CC3)=O)=CC=C2C)=C4N=CC=CN41 |
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 | 16.67 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 333.38. 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 |
|---|---|---|---|
| 0.5 mM | 6 mL | 30 mL | 59.99 mL |
| 2.5 mM | 1.2 mL | 6 mL | 12 mL |
| 5 mM | 0.6 mL | 3 mL | 6 mL |
| 25 mM | 0.12 mL | 0.6 mL | 1.2 mL |
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Product Datasheets
References
References are publications that support the biological activity of the product.
Hohmann and Vakoc et al (2014) A rationale to target the SWI/SNF complex for cancer therapy. Trends Genet. 30 356 PMID: 24932742
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Keywords: TP 472, TP 472 supplier, TP472, bromodomains, BRD9, BRD7, inhibitors, potent, CAS, 2079895-62-6, Bromodomains, 6000, Tocris Bioscience
1 Citation for TP 472
Citations are publications that use Tocris products. Selected citations for TP 472 include:
Gatchalian et al (2018) A non-canonical BRD9-containing BAF chromatin remodeling complex regulates naive pluripotency in mouse embryonic stem cells. Nat Commun 9 5139 PMID: 30510198
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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 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 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 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.