AEM1

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. AEM1 is an inhibitor of gene expression induced by nuclear erythroid 2-related factor 2 (Nrf2). 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.Formal Name: N-(1,3-benzodioxol-5-ylmethyl)-5-(4-fluorophenyl)-thieno[2,3-d]pyrimidin-4-amine. CAS Number: 1030123-90-0. Molecular Formula: C20H14FN3O2S. Formula Weight: 379.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/mL, DMF:PBS (pH 7.2) (1:4): 0.2 mg/mL, DMSO: 20 mg/mL, Ethanol: 0.25 mg/mL. lambdamax: 283 nm. SMILES: FC(C=C1)=CC=C1C2=CSC3=C2C(NCC4=CC=C(OCO5)C5=C4)=NC=N3. InChi Code: InChI=1S/C20H14FN3O2S/c21-14-4-2-13(3-5-14)15-9-27-20-18(15)19(23-10-24-20)22-8-12-1-6-16-17(7-12)26-11-25-16/h1-7,9-10H,8,11H2,(H,22,23,24). InChi Key: QGYLTGSHWIGJJD-UHFFFAOYSA-N.