EPZ015666

SKU: orb1301095

Description

EPZ015666 (GSK3235025) is a potent and selective small molecule inhibitor of protein arginine methyltransferase 5 (PRMT5). It is orally bioavailable and has been utilized in both in vitro and in vivo research to investigate the role of PRMT5 in oncology, hematology, and other disease contexts.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1616391-65-1
• MW: 383.44
• Purity: 99.36%
• Formula: C₂₀H₂₅N₅O₃
• SMILES: O[C@@H](CNC(=O)c1cc(NC2COC2)ncn1)CN1CCc2ccccc2C1
• Target: Histone Methyltransferase
• Solubility: Ethanol:45 mg/mL (117.36 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.22 mM);DMSO:245 mg/mL (638.95 mM)

Bioactivity

• Target IC50:
  PRMT5:5 nM(Ki)
• In Vivo:
  EPZ015666 demonstrates effective cellular activity by blocking the symmetrical dimethylation of SmD3 and inhibiting the proliferation of MCL cell lines, with an IC50 range of 96-904 nM.
• In Vitro:
  Orally administered at a dosage of 200 mg/kg, EPZ015666 exhibits potent antitumor activity in the MCL xenograft animal model.
• Cell Research:
  EPZ015666 is dissolved in DMSO and stored, and then diluted with appropriate medium (final DMSO 0.2%) before use. Cultured cells in linear/log-phase growth are split to a seeding density of 2×105 cells/mL in 2-20 mL of media, depending on the yield required at the end of the growth period. Compound is diluted in DMSO and added to each culture vessel with a final DMSO concentration of 0.2%. Cells are allowed to grow for 96 h undisturbed. At the conclusion of each treatment period, cells are harvested by centrifugation (5 min, 1,200 rpm), and cell pellets are rinsed once with PBS before being frozen on dry ice pending further processing. Long-term proliferation assays are performed on all MCL lines, with slight adjustments to initial seeding densities, depending on growth characteristics for each cell line. All assays are carried out for 12 d.

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

PRMT5, GSK 3235025, GSK3235025, GSK-3235025, EPZ 015666, EPZ015666, EPZ-015666, Inhibitor, Histone Methyltransferase, HistoneMethyltransferase, inhibit

Compound Identifiers

PubChem CID

90241673