Ethaselen - 10mM in DMSO , CAS No.217798-39-5

CAS: 217798-39-5 Cat. No.: E656849 Molecular Weight: 422.20 PubChem CID: 10387485

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Ethaselen (BBSKE) is an orally active, selective thioredoxin reductase (TrxR) inhibitor with IC 50 s of 0.5 and 0.35 μM for the wild-type human TrxR1 and rat TrxR1, respectively. Ethaselen specifically binds to the unique selenocysteine-cysteine redox pair in the C-terminal active site of mammalian TrxR1. Ethaselen, an organoselenium compound, is a potent antitumor candidate that exerts potent inhibition on non-small cell lung cancer (NSCLC) by targeting TrxR

In Vitro

Ethaselen (2.5-10 μM; 12, 24 hours) suppresses A549 cell viability in a both concentration- and time-dependent manner. H1666, which has considerably lower TrxR1 expression level, is less susceptible to 24 h treatment with Ethaselen. Ethaselen inhibits the intracellular TrxR1 activity in a concentration- and time-dependent manner, with IC 50 values of 4.2 and 2 μM for 12- and 24-h treatments, respectively. Ethaselen (2.5-10 μM; 12, 24 hours) has no effect on the protein amounts of TrxR1 and Trx. The mRNA level of TrxR1 does not show significant alteration in Ethaselen-treated A549 cells. Ethaselen (2.5-50 μM; 1-24 hours) causes intracellular Trx oxidation in A549 cells. Ethaselen (5-10 μM; 12, 24 hours) causes a clear concentration-dependent increase in ROS levels in A549 cells. The inhibition constants for Ethaselen binding to free enzyme (K i ) and the enzyme-substrate complex (K is ) were determined to be 0.022 and 0.087 μM, respectively. Ethaselen also inhibits mammalian TrxR1 in a time-dependent manner possibly by forming a covalent Se-S bond with Cys497 of Trx. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: A549 cell Concentration: 2.5, 5, 7.5, 10 μM Incubation Time: 12, 24 hours Result: Suppressed A549 cell viability in a both concentration- and time-dependent manner.

In Vivo

Ethaselen\t(BBSKE; 36-108 mg/kg/day; PO; for 10 days) shows increased inhibition of tumor growth in a dose-independent manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Five-week-old female BALB/c nude mice with A549 cellDosage: 36, 72, 108 mg/kg Administration: PO; daily; for 10 days Result: Showed increased inhibition of tumor growth, and the inhibition levels increased with the dose. The TrxR activity levels of the high dose group (108 mg/kg) decreased more than the middle dose group (72 mg/kg) and low dose group (36 mg/kg).

IC50& Target:TrxR

Specifications

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

Ethaselen (BBSKE) is an orally active, selective thioredoxin reductase (TrxR) inhibitor with IC 50 s of 0.5 and 0.35 μM for the wild-type human TrxR1 and rat TrxR1, respectively. Ethaselen specifically binds to the unique selenocysteine-cysteine redox pai

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Names and Identifiers

• Isomeric SMILES: C1=CC=C2C(=C1)C(=O)N([Se]2)CCN3C(=O)C4=CC=CC=C4[Se]3
• Alternate CAS: 217798-39-5
• PubChem CID: 10387485
• MeSH Entry Terms: (1,2-bis(1,2-benzisoselenazolone-3(2H)-ketone))ethane;BBSKE cpd;ethaselen
• Molecular Weight: 422.20