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GSK2801 is a selective, cell-permeable inhibitor of the BAZ2 family of bromodomain-containing proteins (IC50s = 9-350 nM in a BAZ2B AlphaScreen).1,2 It binds to BAZ2A and BAZ2B with Kd values of 0.26 and 0.14 µM, respectively, and does not interact with the bromodomains of BRD4(BD1), CREBBP, TRIM24/TIF1α, PB1(BD5), PCAF, or ATAD2.1,2 See the Structural Genomics Consortium (SGC) website for more information.
WARNING This product is not for human or veterinary use.
1. Discovery and characterization of GSK2801, a selective chemical probe for the bromodomains BAZ2A and BAZ2B. J. Med. Chem. 59(4), 1410-1424 (2015).
2. Bromodomains and their pharmacological inhibitors. Chem. Med. Chem. 9(3), 438-464 (2014).