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EPZ020411
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
EPZ020411图片
CAS NO:1700663-41-7
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
EPZ020411 是一种选择性的PRMT6抑制剂,其IC50值为10 nM,对 PRMT6 的选择性是 PRMT1 和 PRMT8 的10倍。EPZ020411 可用于癌症的研究。
生物活性

EPZ020411 is a selective inhibitor ofPRMT6with anIC50of 10 nM, has >10 folds selectivity forPRMT6overPRMT1andPRMT8. EPZ020411 can be used for the research ofcancer[1][2].

IC50& Target

PRMT6

0.01 μM (IC50)

PRMT1

0.119 μM (IC50)

PRMT8

0.223 μM (IC50)

体外研究
(In Vitro)

EPZ020411 (0-20 μM; 24 h) decreases H3R2 methylation in A375 cells[1].
EPZ020411 (20-40 μM; 6 h) reduces neomycin- and cisplatin-induced cell apoptosis and increases hair cell survival[2].

Western Blot Analysis[1]

Cell Line:A375 cells
Concentration:0-20 μM
Incubation Time:24 hours
Result:Dose-dependently decreased H3R2 methylation in A375 cells with an IC50of 0.634 μM.

Apoptosis Analysis[2]

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.
体内研究
(In Vivo)

EPZ020411 (10 mg/kg; i.p. once) reduces neomycin- and cisplatin-induced hearing loss in C57BL/6J wild-type mice with acute ototoxicity model[2].
1.19Pharmacokinetic Parameters of EPZ020411 in rats[1].

Rats
IV 1 mg/kg
Rats
SC 5 mg/kg
CL (mL/min/kg)19.7±1.0
Vss(L/kg)11.1±1.6
t1/2(h)8.54±1.439.19±1.60
tmax(h)0.444
Cmax(ng/mL)844±306
AUC0-τ(h·ng/mL)745±342456±135
AUC0-inf(h·ng/mL)846±452775±181
F (%)65.6±4.3

Animal Model:C57BL/6J wild-type mice at P28 with acute ototoxicity model[2]
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.
分子量

442.59

Formula

C25H38N4O3

CAS 号

1700663-41-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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