BRD0539 is a potent inhibitor of Streptococcus pyogenes Cas9 (SpCas9) with IC50 of 22 μM in an in vitro DNA cleavage assay.
BRD0539 is stable in human plasma and reversibly inhibits SpCas9. BRD0539 does not interfere with the SpCas9:gRNA interaction. BRD0539 dose-dependently blocks the formation of the DNA-bound state in a dose-dependent fashion. BRD0539 impairs the perturbation induced by the 4PAM DNA. BRD0539 is able to inhibit SpCas9 in the eGFP-disruption assay.[1]
[1] Basudeb Maji, et al. Cell. 2019 May 2;177(4):1067-1079.e19.
















