EPZ020411

SKU: orb1225961

Description

EPZ020411 is a potent, selective PRMT6 inhibitor with IC50 of 10 nM, displays 10-fold and 20-fold selectivity over PRMT1/8, and >100-fold over other histone methyltransferases (PRMT3/4/5/7); dose-dependently decreases H3R2 methylation A375 cell line with IC50 of 0.637 uM, with no affect levels of PRMT6 expression; exhibits good bioavailability following subcutaneous dosing in rats making it a suitable tool for potential in vivo target validation studies.

Key Properties

• CAS Number: 1700663-41-7
• MW: 442.5942
• Purity: >98% (HPLC)
• Formula: C₂₅H₃₈N₄O₃
• SMILES: CNCCN(C)CC1=C(NN=C1)C2=CC=C(C=C2)OC3CC(C3)OCCC4CCOCC4
• Target: HMTase
• Solubility: 10 mM in DMSO

Bioactivity

• 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. Pharmacokinetic Parameters of EPZ020411 in rats. Animal model: C57BL/6J wild-type mice at P28 with acute ototoxicity model. 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.
• 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. Western blot analysis. Cell line: A375 cells. Concentration: 0-20 μM. Incubation time: 24 hours. Result: Dose-dependently decreased H3R2 methylation in A375 cells with an IC50 of 0.634 μM. Apoptosis Analysis 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

EPZ-020411

Quick Database Links

Gene Symbol

HMTase