BRD0639 是首创的PRMT5-substrate adaptor interaction的抑制剂。BRD0639 是一种 PRMT5 结合基序 (PBM) 竞争性抑制剂，可以支持 PBM 依赖的 PRMT5 活性的研究。

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

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 bind the cellular target and potently outcompete binding between full-length PRMT5 and RIOK1 proteins with an IC 50 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].

T9329

C21H22ClN5O4S

475.95

DMSO:60 mg/ml (126.06 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years