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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 for GSK 2801
GSK 2801 is a 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 for GSK 2801
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 for GSK 2801
| 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 for GSK 2801
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 18.57 | 50 |
Preparing Stock Solutions for GSK 2801
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 for GSK 2801
References for GSK 2801
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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