PeptideDB

EPZ020411

CAS: 1700663-41-7 F: C25H38N4O3 W: 442.59

EPZ020411 is a selective inhibitor of PRMT6 with an IC50 of 10 nM, has >10 folds selectivity for PRMT6 over PRMT1 and PR
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This product is for research use only, not for human use. We do not sell to patients.

Bioactivity EPZ020411 is a selective inhibitor of PRMT6 with an IC50 of 10 nM, has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 can be used for the research of cancer[1][2].
Invitro 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:
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].
Name EPZ020411
CAS 1700663-41-7
Formula C25H38N4O3
Molar Mass 442.59
Transport Room temperature in continental US; may vary elsewhere.
Storage

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

Reference [1]. Mitchell LH, et al. Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 ToolCompound. ACS Med Chem Lett. 2015 Apr 6;6(6):655-659. [2]. He Y, et al. Inhibition of Protein arginine methyltransferase 6 reduces reactive oxygen species production and attenuates aminoglycoside- and cisplatin-induced hair cell death. Theranostics. 2020 Jan 1;10(1):133-150.