EPZ020411 hydrochloride is a selective inhibitor of PRMT6 with an IC50 of 10 nM, it has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 hydrochloride can be used for the research of cancer[1][2].
EPZ020411 hydrochloride (0-20 μM; 24 h) decreases H3R2 methylation in A375 cells[1].
EPZ020411 hydrochloride (20-40 μM; 6 h) reduces neomycin- and cisplatin-induced cell apoptosis and increases hair cell survival[2].
EPZ020411 hydrochloride (10 mg/kg; i.p. once) reduces neomycin- and cisplatin-induced hearing loss in C57BL/6J wild-type mice with acute ototoxicity model[2].
1.19
Pharmacokinetic Parameters of EPZ020411 hydrochloride in rats[1].
RatsIV 1 mg/kg
RatsSC 5 mg/kg
CL (mL/min/kg)
19.7±1.0
Vss (L/kg)
11.1±1.6
t1/2 (h)
8.54±1.43
9.19±1.60
tmax (h)
0.444
Cmax (ng/mL)
844±306
AUC0-τ (h·ng/mL)
745±34
2456±135
AUC0-inf (h·ng/mL)
846±45
2775±181
F (%)
65.6±4.3
| Catalog Number | I005793 |
| CAS Number | 2070015-25-5 |
| Synonyms | N,N’-dimethyl-N’-[[5-[4-[3-[2-(oxan-4-yl)ethoxy]cyclobutyl]oxyphenyl]-1H-pyrazol-4-yl]methyl]ethane-1,2-diamine;hydrochloride |
| Molecular Formula | C25H39ClN4O3 |
| Purity | 95% |
| InChI | InChI=1S/C25H38N4O3.ClH/c1-26-10-11-29(2)18-21-17-27-28-25(21)20-3-5-22(6-4-20)32-24-15-23(16-24)31-14-9-19-7-12-30-13-8-19;/h3-6,17,19,23-24,26H,7-16,18H2,1-2H3,(H,27,28);1H |
| InChIKey | LIDZHJMYAKPGOJ-UHFFFAOYSA-N |
| SMILES | CNCCN(C)CC1=C(NN=C1)C2=CC=C(C=C2)OC3CC(C3)OCCC4CCOCC4.Cl |
| 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. |
