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Submit ReviewGSK 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.
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.
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.
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.
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
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
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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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.
This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.