For research use only.

Catalog No.S8844

1 publication

BRD0539 Chemical Structure

CAS No. 1403838-79-8

BRD0539 is a potent inhibitor of Streptococcus pyogenes Cas9 (SpCas9) with IC50 of 22 μM in an in vitro DNA cleavage assay.

Selleck's BRD0539 has been cited by 1 publication

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Biological Activity

Description BRD0539 is a potent inhibitor of Streptococcus pyogenes Cas9 (SpCas9) with IC50 of 22 μM in an in vitro DNA cleavage assay.
SpCas9 [1]
(Cell-free assay)
22 μM
In vitro

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]


Cell Research:


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  • Cell lines: U2OS.eGFP.PEST cells
  • Concentrations: 15 μM
  • Incubation Time: 2–24 h
  • Method:

    The reversal of BRD0539-mediated inhibition of SpCas9 is performed using the eGFP-disruption assay, wherein 2×105 U2OS.eGFP.PEST cells are nucleofected with preformed SpCas9:gRNA complex. Approximately 22,000 transfected cells/well are plated in four replicates in a 96-well plate along with 15 μM of BRD0539 or DMSO. For AcrIIA4 reversibility experiments, a preformed SpCas9:gRNA (10 pmol) is incubated with AcrIIA4 (5×) for 10 min and then is nucleofected to U2OS.eGFP.PEST cells following the aforementioned protocol. The media is swapped with fresh media containing no BRD0539/AcrIIA4 at the indicated time point (2–24 h), and the cells are allowed to grow until 24 h post-nucleofection.

    (Only for Reference)

Solubility (25°C)

In vitro DMSO 91 mg/mL (201.08 mM)
Water Insoluble
Ethanol ''31 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 452.54


CAS No. 1403838-79-8
Storage powder
in solvent
Synonyms N/A
Smiles CC1=CC=C(C=C1)S(=O)(=O)N2CCC3C2C4=C(C=CC(=C4)C5=CC=CC=C5F)NC3CO

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID