Home Epigenetics PRMT inhibitor BRD0639

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BRD0639 PRMT inhibitor

Cat.No.E1007

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 PRMT inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 475.948

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Quality Control

Batch: E100701 DMSO]95 mg/mL]false]Ethanol]95 mg/mL]false]Water]Insoluble]false Purity: 99.56%
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  • COA
  • NMR
  • HPLC
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  • Datasheet
99.56

Solubility

In vitro
Batch:

DMSO : 95 mg/mL (199.6 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 95 mg/mL

Water : Insoluble

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In vivo
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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 475.948 Formula

C21H22ClN5O4S

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 2760881-74-9 -- Storage of Stock Solutions

Synonyms N/A Smiles CC(N1N=CC(=CC1=O)Cl)C(=O)NC2=CC=C(C)C(=C2)[S](=O)(=O)NCCC3=NC=CC=C3

Mechanism of Action

Targets/IC50/Ki
PRMT5-RIOK1 complex
(in permeabilized cells)
7.5 μM
PRMT5-RIOK1 complex
(in permeabilized cells)
16 μM
In vitro

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

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