Background
LP99 is a potent inhibitor of the bromodomain containing proteins BRD7 and BRD9 that binds with Kd values of 99 and 909 nM, respectively, as determined by isothermal titration calorimetry. It is selective for BRD7/9 over a panel of 48 BRDs at concentrations up to 10 uM determined using differential scanning fluorimetry. It inhibits BRD7 interactions with histones H3.3 and H4 with IC50 values of 3.7 and 3.3 uM, respectively, in a bioluminescence resonance energy transfer (BRET) assay in HEK293 cells. Similarly, it inhibits BRD9 from interacting with H3.3 and H4 with IC50 values of 5.1 and 6.2 uM, respectively. It also decreases the level of IL-6 secreted from LPS-stimulated THP-1 cells. See the Structural Genomics Consortium (SGC) website for more information.
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