EPZ020411 hydrochloride

SKU: orb1704829

Description

EPZ020411 hydrochloride is a potent and selective PRMT6 inhibitor exhibiting an IC50 of 10 nM. This compound is a valuable research tool for investigating the role of PRMT6 in epigenetic regulation, cancer biology, and other cellular processes in both in vitro and in vivo experimental models.

Research Area

Cell Biology, Epigenetics & Chromatin

Key Properties

• CAS Number: 2070015-25-5
• MW: 479.05
• Purity: >99.99% (May vary between batches)
• Formula: C₂₅H₃₉ClN₄O₃
• SMILES: Cl.CNCCN(C)Cc1c[nH]nc1-c1ccc(O[C@H]2C[C@@H](C2)OCCC2CCOCC2)cc1
• Target: Histone Methyltransferase,Apoptosis
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.17 mM);H2O:18 mg/mL (37.57 mM);DMSO:45 mg/mL (93.94 mM)

Bioactivity

• Target IC50:
  PRMT6:10 nM|PRMT1:119 nM|PRMT8:223 nM
• In Vivo:
  EPZ020411 shows good bioavailability following subcutaneous dosing in rats. Male Sprague-Dawley rats administered EPZ020411 at a single dose of 1 mg/kg by i.v. bolus show a moderate clearance (CL) of 19.7±1.0 mL/min/kg, with a volume of distribution at steady state (Vss) of 11.1±1.6 L/kg, translating to a mean terminal half-life (t1/2) of 8.54±1.43 h. A good bioavailability of 65.6 ± 4.3% is observed following 5 mg/kg s.c. dosing, leading to EPZ020411 unbound blood concentration remaining above the PRMT6 biochemical IC50 for more than 12 h.
• In Vitro:
  Treatment with EPZ020411 results in a dose-dependent decrease in H3R2 methylation in A375 human melanoma cells exogenously overexpressing PRMT6(IC50=0.637±0.241 μM). EPZ020411 is over 100-fold selective for PRMT6/8/1 compared to other histone methyltransferases including PRMT3, PRMT4, PRMT5, and PRMT7 in biochemical assays. The compound shows poor permeability in the parallel artificial membrane permeation assay.
• Cell Research:
  Cell lines: A375 cells. Concentrations: 0-20 μM. Incubation Time: 48 h. Method: A375 (CRL-1619) cells are cultured in DMEM with 10% (vol/vol) FBS. PRMT6 is cloned into EcoRI and BamHI sites of a pcDNA4 HisMAX_A plasmid. According to procedures recommended by the manufacturer, transfection of his-tagged PRMT6 or vector control is carried out using Lipofectamine LTX and Plus reagent . Cells are seeded at 200,000 cells/well in 6-well plates. The second day, the cells are concurrently transfected and treated with compound in 0.25% DMSO. Cells are incubated in the presence compound at 20 μM and collected after 48 hours treatment.
• Animal Research:
  Animal Models: SD rats. Dosages: 1 mg/kg. Administration: i.v..

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PRMT1, PRMT6, PRMT8, EPZ020411 HCl, EPZ 020411 Hydrochloride, EPZ020411 Hydrochloride, EPZ020411 hydrochloride, EPZ-020411 hydrochloride, EPZ-020411 Hydrochloride, HistoneMethyltransferase, Histone Methyltransferase

Compound Identifiers

PubChem CID

119081410