EPZ-015866

SKU: orb1226051

Description

EPZ-015866 (GSK-591, GSK-3203591) is a potent, selective protein methyltransferase 5 (PRMT5) inhibitor with IC50 of 4 nM; shows excellent selectivity against other PMT enzymes observed with EPZ015666; inhibits the proliferation of Z-138 cells with IC50 of 62 nM.

Key Properties

• CAS Number: 1616391-87-7
• MW: 380.4833
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₈N₄O₂
• SMILES: O=C(NC[C@H](O)CN1CCC(C=CC=C2)=C2C1)C3=CC(NC4CCC4)=NC=C3
• Target: HMTase
• Solubility: 10 mM in DMSO

Bioactivity

• In Vitro:
  GSK591 (5 μM; MCF7, T47D, and MCF10A cells) treatment suppresses breast cancer stem cells (BCSCs) proliferation and self-renewal. GSK591 reduces BCSCs numbers in vitro. Cell Proliferation Assay Cell line: MCF7, T47D, and MCF10A cells. Concentration: 5 μM. Incubation time: Result: Suppressed BCSCs proliferation and self-renewal.

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

GSK-591 | GSK-3203591

Quick Database Links

Gene Symbol

HMTase