Home DNA Damage/DNA Repair CRISPR/Cas9 inhibitor BRD0539 For research use only.

BRD0539

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

BRD0539 Chemical Structure

CAS: 1403838-79-8

Selleck's BRD0539 has been cited by 1 publication

Purity & Quality Control

Batch: S884401 DMSO] 91 mg/mL] false] Ethanol] 31 mg/mL] false] Water] Insoluble] false Purity: 98.09%
98.09

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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
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 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.

Chemical Information & Solubility

Molecular Weight 452.54 Formula

C25H25FN2O3S
CAS No. 1403838-79-8 SDF --
Smiles CC1=CC=C(C=C1)S(=O)(=O)N2CCC3C2C4=C(C=CC(=C4)C5=CC=CC=C5F)NC3CO
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 91 mg/mL ( (201.08 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 31 mg/mL

Water : Insoluble


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In vivo
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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. )

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

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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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