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. |