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) |
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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. |
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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±1.43 | 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 |
| 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. |
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| 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. |
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