EPZ020411 is a selective inhibitor of PRMT6 with an IC 50 of 10 nM, has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8 . EPZ020411 can be used for the research of cancer In Vitro 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: A375 cells Concentration: 0-20 μM Incubation Time: 24 hours Result: Dose-dependently decreased H3R2 methylation in A375 cells with an IC 50 of 0.634 μM. Apoptosis AnalysisCell 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. 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. 1.19 Pharmacokinetic Parameters of EPZ020411 in rats . Rats IV 1 mg/kg Rats SC 5 mg/kg CL (mL/min/kg) 19.7±1.0 V ss (L/kg) 11.1±1.6 t 1/2 (h) 8.54±1.43 9.19±1.60 t max (h) 0.444 C max (ng/mL) 844±306 AUC 0-τ (h·ng/mL) 745±34 2456±135 AUC 0-inf (h·ng/mL) 846±45 2775±181 F (%) 65.6±4.3 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57BL/6J wild-type mice at P28 with acute ototoxicity modelDosage: 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. IC50& Target:PRMT6 0.01 μM (IC 50 ) PRMT1 0.119 μM (IC 50 ) PRMT8 0.223 μM (IC 50 )
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EPZ020411
CAS number：1700663-41-7 molecular formula：C25H38N4O3
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 1700663-41-7 | molecular formula | C25H38N4O3 |
| molecular weight | 442.6 g/mol | Exact mass | - |
| PSA | 71.600 Ų | logp | 2.700 |
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