BRD0539

Names

[ Name ]:
BRD0539

Biological Activity

[Description]:

BRD0539 is a cell-permeable and non-toxic inhibitor of CRISPR-Cas9. BRD0539 inhibits Streptococcus pyogenes Cas9 (SpCas9) (apparent IC50=22 μM) in an in vitro DNA cleavage assay[1].

[Related Catalog]:

Research Areas >> Infection

Signaling Pathways >> Cell Cycle/DNA Damage >> CRISPR/Cas9

[Target]

IC50: 22 μM (SpCas9)[1]

[In Vitro]

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[1]. BRD0539 does not interfere with the SpCas9:gRNA interaction[1]. BRD0539 is able to inhibit SpCas9 in the eGFP-disruption assay, BRD0539 is unable to inhibit FnCpf1, a structurally different CRISPR-associated nuclease, in the same assay, further highlighting the specificity of BRD0539[1].

[References]

[1]. Basudeb Maji, et al. A High-Throughput Platform to Identify Small-Molecule Inhibitors of CRISPR-Cas9. Cell. 2019 May 2;177(4):1067-1079.e19.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₅H₂₅FN₂O₃S

[ Molecular Weight ]:
452.54

Related Compounds

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