A BRD9 bromodomain inhibitor
pIC50: 7.3
I-BRD9 is a BRD9 inhibitor.
BRD9 is identified as a bromodomain containing protein forming a small sub-branch of the bromodomain family tree. Human BRD9 has a single bromodomain and contains five isoforms which are produced by alternative splicing.
In vitro: In previous study, the I-BRD9 development was driven by iterative medicinal chemistry, using structure based design to result in nanomolar potency at BRD9, over 700-fold selectivity against the BET family as well as more than 70-fold to a panel of 34 bromodomains. In Kasumi-1 cells, I-BRD9 could downregulate DUSP6, CLEC1, SAMSN1 and FES genes. Moreover, I-BRD9 was used to expore genes regulated by BRD9 in Kasumi-1 cells involved in immune response and oncology pathways. In addition, when BRD4 was used as a representative member of the BET family for initial selectivity screening, I-BRD9 was found to have a pIC50 of 5.3 against this protein. I-BRD9 thus represented the first available selective tool compound to investigate the cellular phenotype of the inhibition of BRD9 bromodomain [1].
In vivo: So far, there is no animal in vivo data reported for I-BRD9.
Clinical trial: Up to now, I-BRD9 is still in the preclinical development stage.
Reference:
[1] Theodoulou NH et al.? Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition. J Med Chem. 2016 Feb 25;59(4):1425-39.
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