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Submit ReviewGSK 2801
Description: Selective BAZ2A and BAZ2B inhibitor
Chemical Name: 1-[1-[2-(Methylsulfonyl)phenyl]-7-propoxy-3-indolizinyl]ethanone
Purity: ≥98% (HPLC)
Biological Activity
Selective BAZ2A and BAZ2B inhibitor (IC50 values are 0.40 and 0.43 μM, respectively). Selective for BAZ2A/B over TAF1L and BRD9. Cell permeable and orally available.
Licensing Information
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the GSK 2801 probe summary on the SGC website.
External Portal Information
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of GSK2801 is reviewed on the chemical probes website.
Technical Data
| M. Wt | 371.45 |
| Formula | C20H21NO4S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1619994-68-1 |
| PubChem ID | 73010930 |
| InChI Key | KHWCPNJRJCNVRI-UHFFFAOYSA-N |
| Smiles | CCCOC1=CC2=C(C3=C(S(C)(=O)=O)C=CC=C3)C=C(C(C)=O)N2C=C1 |
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 | 18.57 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 371.45. 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 | 5.38 mL | 26.92 mL | 53.84 mL |
| 2.5 mM | 1.08 mL | 5.38 mL | 10.77 mL |
| 5 mM | 0.54 mL | 2.69 mL | 5.38 mL |
| 25 mM | 0.11 mL | 0.54 mL | 1.08 mL |
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Product Datasheets
References
References are publications that support the biological activity of the product.
Chen et al (2015) Discovery and characterization of GSK2801, a selective chemical probe for the bromodomains BAZ2A and BAZ2B. J.Med.Chem PMID: 25799074
If you know of a relevant reference for GSK 2801, please let us know.
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Keywords: GSK 2801, GSK 2801 supplier, selective, bromodomain, inhibitors, inhibits, cell, permeable, orally, bioavailable, BAZ2A, BAZ2B, structural, genomics, consortium, SGC, GSK2801, Bromodomains, 5635, Tocris Bioscience
Citations for GSK 2801
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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.