BRD9757 is a highly potent and selective HDAC6 inhibitor with an IC₅₀ of 30 nM toward HDAC6. It has >20-fold selectivity for class I and > 400-fold selectivity for class II HDACs tested. BRD9757 is absence of a surface-binding motif. It demonstrates that high selectivity and potent inhibition of HDAC6 can be achieved through careful choice of linker element only. BRD9757 can be used as a useful tool for probing the biological functions and relevance of the different HDAC isoforms, and serves as a basis for new selective inhibitors of other HDAC isoforms.

How to Use:

In vitro:  BRD9757 was suggested to be used at 10 µM final concentration in vitro and in cellular assays.

In vivo:  n/a

Reference:

1. 1. Wagner FF, et al. Potent and Selective Inhibition of Histone Deacetylase 6 (HDAC6) Does Not Require a Surface-Binding Motif. (2013) J Med Chem. 56 (4), 1772–1776.

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