BRD0539

Catalog No.S8844

For research use only.

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

BRD0539 Chemical Structure

CAS No. 1403838-79-8

Selleck's BRD0539 has been cited by 1 Publication

Purity & Quality Control

Choose Selective CRISPR/Cas9 Inhibitors

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.
Targets
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]

Protocol (from reference)

Cell Research:

[1]

  • 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.

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 452.54
Formula

C25H25FN2O3S

CAS No. 1403838-79-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC=C(C=C1)S(=O)(=O)N2CCC3C2C4=C(C=CC(=C4)C5=CC=CC=C5F)NC3CO

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Tech Support

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.

Handling Instructions

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