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.
Storage Temp
Store at -80°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of protein arginine methyltransferase 6
Product Description
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.
This compound belongs to the class of organic compounds known as phenylpyrazoles. These are compounds containing a phenylpyrazole skeleton, which consists of a pyrazole bound to a phenyl group.
External Descriptors
Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
