An inhibitor of Nrf2-induced gene expression; reduces Nrf2-dependent expression of the genes encoding SOD1

AEM1 – 1 mg

Brand:
Cayman
CAS:
1030123-90-0
Storage:
-20
UN-No:
Non-Hazardous - /

Cancer cell survival appears partly dependent on antioxidative enzymes, whose expression is regulated by the Keap1-Nrf2 pathway, to quench potentially toxic reactive oxygen species generated by their metastatic transformation.{20112} AEM1 is an inhibitor of gene expression induced by nuclear erythroid 2-related factor 2 (Nrf2).{29333} It reduces Nrf2-dependent expression of the genes encoding superoxide dismutase 1 (SOD1), heme oxygenase 1 (HO-1), thioredoxin (Trx), glutamate-cysteine ligase (GCLM), and glutathione peroxidase 2 (GPX2), as well as decreases glutathione (GSH) content in A549 cells when used at 5 µM. AEM1 enhances tert-butyl hydroperoxide-induced A549 cell death. In vivo, AEM1 (50 mg/kg) reduces tumor volume in an A549 mouse xenograft model.  

 

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Description

An inhibitor of Nrf2-induced gene expression; reduces Nrf2-dependent expression of the genes encoding SOD1, HO-1, Trx, GCLM, and GPX2, as well as decreases GSH content in A549 cells at 5 µM; enhances tert-butyl hydroperoxide-induced A549 cell death; reduces tumor volume in an A549 mouse xenograft model at 50 mg/kg

Formal name: N-(1,3-benzodioxol-5-ylmethyl)-5-(4-fluorophenyl)-thieno[2,3-d]pyrimidin-4-amine

Synonyms: 

Molecular weight: 379.4

CAS: 1030123-90-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals||Research Area|Cancer|Cell Death||Research Area|Cancer|Transcription Factors||Research Area|Oxidative Stress & Reactive Species|Pro-oxidant Activity||Research Area|Oxidative Stress & Reactive Species|Reactive Sulfur|Glutathione

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