EPZ020411

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

EPZ020411 是一种有效的选择性 PRMT6 抑制剂，IC50 为 10 nM。

EPZ020411 is a potent, selective PRMT6 inhibitor with IC50 of 10 nM, displays 10-fold and 20-fold selectivity over PRMT1/8, and >100-fold over other histone methyltransferases (PRMT3/4/5/7); dose-dependently decreases H3R2 methylation A375 cell line with IC50 of 0.637 uM, with no affect levels of PRMT6 expression; exhibits good bioavailability following subcutaneous dosing in rats making it a suitable tool for potential in vivo target validation studies.

EPZ020411 (0-20 μM; 24 h) decreases H3R2 methylation in A375 cells.EPZ020411 (20-40 μM; 6 h) reduces neomycin- and cisplatin-induced cell apoptosis and increases hair cell survival. Western Blot Analysis Cell Line:A375 cells Concentration:0-20 μM Incubation Time:24 hours Result:Dose-dependently decreased H3R2 methylation in A375 cells with an IC50 of 0.634 μM.Apoptosis Analysis Cell Line:Cultured cochleae cells Concentration:20-40 μM Incubation Time:6 hours Result:Suppressed the apoptotic cascade induced by aminoglycosides and also inhibited cisplatin-induced apoptosis in the hair cells of the cochlear explants after pretreatment deposed. Also reduced hair cell loss caused by cisplatin treatment.

EPZ020411 (10 mg/kg; i.p. once) reduces neomycin- and cisplatin-induced hearing loss in C57BL/6J wild-type mice with acute ototoxicity model.Pharmacokinetic Parameters of EPZ020411 in rats. Animal Model:C57BL/6J wild-type mice at P28 with acute ototoxicity model Dosage:10 mg/kg Administration:Intraperitoneal injection; 10 mg/kg once Result:Significantly reduced neomycin- and cisplatin-induced HC loss and showed no effect without neomycin injection with mice.

EPZ-020411

Chromatin/Epigenetic

HMTase

PRMT6

Other Indications

——

1700663-41-7

442.5942

C25H38N4O3

>98% (HPLC)

10 mM in DMSO

CNCCN(C)CC1=C(NN=C1)C2=CC=C(C=C2)OC3CC(C3)OCCC4CCOCC4

1,2-Ethanediamine, N1,N2-dimethyl-N1-[[3-[4-[[trans-3-[2-(tetrahydro-2H-pyran-4-yl)ethoxy]cyclobutyl]oxy]phenyl]-1H-pyrazol-4-yl]methyl]-

(-20℃)

With Ice Pack

≥ 2 years