EI1

SKU: orb1300728

Description

EI1 is a potent and selective small molecule inhibitor of EZH2, demonstrating IC50 values of 15 nM against wild-type and 13 nM against the Y641F mutant. It is widely used in vitro and in vivo to study epigenetic mechanisms in oncology, particularly for cancers driven by EZH2 dysregulation such as lymphomas.

Research Area

Cell Biology, Epigenetics & Chromatin

Key Properties

• CAS Number: 1418308-27-6
• MW: 390.48
• Purity: 99.98% (May vary between batches)
• Formula: C₂₃H₂₆N₄O₂
• SMILES: CCC(CC)n1ccc2c(cc(cc12)C#N)C(=O)NCc1c(C)cc(C)[nH]c1=O
• Target: Apoptosis,Histone Methyltransferase
• Solubility: H2O:Insoluble;DMSO:12.5 mg/mL (32.01 mM)

Bioactivity

• Target IC50:
  EZH2 (WT):15 nM|EZH2 (Y641F):13 nM
• In Vitro:
  In DLBCL cells, EI1 inhibits cellular H3K27 methylation and activates Ezh2 target gene p16 expression. In mouse embryonic fibroblasts, EI1 also inhibit H3K27me3 and cell proliferation. In addition, EI1 selectively inhibits the growth of DLBCL cells carrying Ezh2 mutation, and causes cell cycle arrest and apoptosis.
• Cell Research:
  Exponentially growing diffused large B-cell lymphoma (DLBCL) cells are seeded in 12-well plates at a density of 1 × 105 cells/mL with the indicated concentration of EI1. Viable cell number is determined every 3–4 d for up to 14 or 15 d by Vi-CELL. Mouse embryonic fibroblasts (MEFs) are seeded in a six-well plate at 2.5 × 104 cell/mL and treated with EI1 (3.3 μM) or 4-OH-tamoxifen (100 nM). Viable cell number is determined at days 3, 6 and 11. On days of cell counts, fresh growth medium and compound are replenished and cells split back to a density of 1 × 105 cells/mL. Total cell number is expressed as split-adjusted viable cells per milliliter. IC50 is calculated by PRISM and all proliferation experiments are repeated more than two times and representative data are presented.(Only for Reference)

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

Apoptosis, inhibit, KB 145943, KB145943, KB-145943, EI 1, EI1, EI-1, EZH2, Ezh2 inhibitor, Inhibitor, HistoneMethyltransferase, Histone Methyltransferase

Compound Identifiers

PubChem CID

72199293