BRD0639

Catalog No.E1007

For research use only.

BRD0639 is a first-in-class PBM-competitive small molecule inhibitor that disrupts the PRMT5-RIOK1 complex with IC50s of 7.5 μM and 16 μM in permeabilized and living cells, respectively.

BRD0639 Chemical Structure

CAS No.

Purity & Quality Control

Choose Selective PRMT Inhibitors

Biological Activity

Description

BRD0639 is a first-in-class PBM-competitive small molecule inhibitor that disrupts the PRMT5-RIOK1 complex with IC50s of 7.5 μM and 16 μM in permeabilized and living cells, respectively.

Targets
PRMT5-RIOK1 complex [1]
(in permeabilized cells)
PRMT5-RIOK1 complex [1]
(in permeabilized cells)
7.5 μM 16 μM
In vitro

BRD0639, which engages the target in Expi293 cells, disrupts PRMT5−RIOK1 complexes, and reduces substrate methylation. BRD0639 also reduces SDMA in the same subset of proteins affected by genetic perturbation of the PBM binding site.[1]

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: Expi293 cells
  • Concentrations: 25 μM
  • Incubation Time: 12 h
  • Method:

    Cells are plated at 1 × 106/well in 6-well tissue culture treated plates and treated the next day with BRD0639 to a final concentration of 25 μM. Twelve h after treatment, the media is refreshed and cells retreated. Twelve h later, cells are washed 1× with PBS and lysed on ice for 15 min in 50 μL lysis buffer.

  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 95 mg/mL
(199.6 mM)
Ethanol 95 mg/mL
(199.6 mM)
Water 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.

Chemical Information

Molecular Weight 475.948
Formula

C21H22ClN5O4S

CAS No.
Storage 3 years -20°C powder
2 years -80°C in solvent

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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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