For research use only. Not for therapeutic Use.
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 Nrf2-induced gene transcription at the antioxidant response element in cells at 1 to 10 µM. It sensitizes lung carcinoma A549 cells to chemotherapeutic agents and inhibits the growth of A549 cells <em>in vitro</em> and <em>in vivo</em> in animals. The effectiveness of AEM1 against cancer cells is restricted to those harboring mutations that render Nrf2 constitutively active.
| Catalog Number | R065768 |
| CAS Number | 1030123-90-0 |
| Synonyms | N-(1,3-benzodioxol-5-ylmethyl)-5-(4-fluorophenyl)-thieno[2,3-d]pyrimidin-4-amine |
| Molecular Formula | C20H14FN3O2S |
| Purity | ≥95% |
| Target | Keap1-Nrf2 |
| Storage | -20°C |
| IUPAC Name | N-(1,3-benzodioxol-5-ylmethyl)-5-(4-fluorophenyl)thieno[2,3-d]pyrimidin-4-amine |
| InChI | 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) |
| InChIKey | QGYLTGSHWIGJJD-UHFFFAOYSA-N |
| SMILES | C1OC2=C(O1)C=C(C=C2)CNC3=C4C(=CSC4=NC=N3)C5=CC=C(C=C5)F |
| Reference | 1.DeNicola, G.M.,Karreth, F.A.,Humpton, T.J., et al. Oncogene-induced Nrf2 transcription promotes ROS detoxification and tumorigenesis. Nature 475(7354), 106-109 (2011). |
