BRD0539

Catalog No.S8844 Batch:S884401

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Technical Data

Formula

C25H25FN2O3S
Molecular Weight 452.54 CAS No. 1403838-79-8
Solubility (25°C)* In vitro DMSO 91 mg/mL (201.08 mM)
Ethanol 31 mg/mL (68.5 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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.
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 Assay:

[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.

Selleck's BRD0539 has been cited by 1 publication

Targeting KDM4A epigenetically activates tumor-cell-intrinsic immunity by inducing DNA replication stress [ Mol Cell, 2021, S1097-2765(21)00168-4] PubMed: 33743195

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.