Home Epigenetics PRMT inhibitor BRD0639 For research use only.

BRD0639

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

BRD0639 Chemical Structure

CAS: 2760881-74-9

Purity & Quality Control

Batch: E100701 DMSO] 95 mg/mL] false] Ethanol] 95 mg/mL] false] Water] Insoluble] false Purity: 99.56%
99.56

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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
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]
Cell Research 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.

Chemical Information & Solubility

Molecular Weight 475.948 Formula

C21H22ClN5O4S
CAS No. 2760881-74-9 SDF --
Smiles CC(N1N=CC(=CC1=O)Cl)C(=O)NC2=CC=C(C)C(=C2)[S](=O)(=O)NCCC3=NC=CC=C3
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 95 mg/mL ( (199.6 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 95 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. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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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