1. Epigenetics
  2. Histone Methyltransferase
  3. BRD0639

BRD0639 

Cat. No.: HY-132309
Handling Instructions

BRD0639 is a first-in-class inhibitor of the PRMT5-substrate adaptor interaction. BRD0639 is a PRMT5 binding motif (PBM)-competitive agent that can support studies of PBM dependent PRMT5 activities.

For research use only. We do not sell to patients.

BRD0639 Chemical Structure

BRD0639 Chemical Structure

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Description

BRD0639 is a first-in-class inhibitor of the PRMT5-substrate adaptor interaction. BRD0639 is a PRMT5 binding motif (PBM)-competitive agent that can support studies of PBM dependent PRMT5 activities[1].

In Vitro

BRD0639 is a first-in-class PBM-competitive small molecule that can support studies of PBM dependent PRMT5 activities and the development of novel PRMT5 inhibitors that selectively target these functions. BRD0639 can engage the cellular target and effectively outcompete binding between full-length PRMT5 and RIOK1 proteins with an IC50 of 7.5 uM and 16 uM in permeabilized and living cells, respectively. BRD0639 reduces SDMA in the same subset of proteins also affected by genetic perturbation of the PRMT5 binding motif (PBM) binding site[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

475.95

Formula

C₂₁H₂₂ClN₅O₄S

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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BRD0639
Cat. No.:
HY-132309
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