Ethaselen

SKU: orb1691145

Description

Ethaselen (BBSKE) is an orally bioavailable, selective inhibitor of thioredoxin reductase 1 (TrxR1). It demonstrates anticancer activity by inducing apoptosis and inhibiting proliferation, particularly in colorectal cancer models, and shows synergistic effects when combined with oxaliplatin in both in vitro and in vivo studies.

Research Area

Metabolism Research

Key Properties

• CAS Number: 217798-39-5
• MW: 422.2
• Purity: 99.14%
• Formula: C₁₆H₁₂N₂O₂Se₂
• SMILES: O=C1C=2C=CC=CC2[Se]N1CCN3[Se]C=4C=CC=CC4C3=O
• Target: Reductase
• Solubility: 10% DMSO+90% Corn Oil:1 mg/mL (2.37 mM);DMSO:10 mg/mL (23.69 mM)

Bioactivity

• In Vivo:
  In A549 cells, using five-week-old female BALB/c nude mice as the experimental model, treatment with Ethaselen (36, 72, 108 mg/kg; PO; daily; for 10 days) resulted in increased inhibition of tumor growth, with inhibition levels increasing with the dose. The high-dose group (108 mg/kg) exhibited a greater decrease in TrxR activity levels compared to the middle-dose group (72 mg/kg) and low-dose group (36 mg/kg).
• In Vitro:
  Ethaselen (2.5-10 μM; 12, 24 hours) diminishes A549 cell viability in a concentration- and time-dependent manner. H1666 cells, with lower TrxR1 expression, show reduced sensitivity to Ethaselen after 24 hours. Ethaselen selectively inhibits TrxR1 activity (IC50: 4.2 and 2 μM for 12 and 24 hours) without altering TrxR1 or Trx protein levels or TrxR1 mRNA in A549 cells. Additionally, Ethaselen (2.5-50 μM; 1-24 hours) induces Trx oxidation and increases ROS levels in A549 cells at 5-10 μM (12, 24 hours). The inhibition constants (K_i and K_is) are 0.022 and 0.087 μM, respectively, suggesting Ethaselen impedes mammalian TrxR1 possibly by forming a covalent bond with Cys497 of Trx in a time-dependent manner. A Cell Viability Assay confirms Ethaselen’s effectiveness in suppressing A549 cell viability at 2.5-10 μM over 12 and 24 hours, reinforcing its concentration and time dependency.

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

BBSKE, TrxR

Compound Identifiers

PubChem CID

10387485