An inhibitor of Nrf2-induced gene expression
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AEM1

Item No. 18321

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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(Learn about Variance in Solubility)
DMF: 30 mg/mLDMF:PBS (pH 7.2) (1:4): 0.2 mg/mLDMSO: 20 mg/mLEthanol: 0.25 mg/mL
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

    $203

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    Cayman Chemical
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    Product Description

    AEM1 is an inhibitor of gene expression induced by nuclear erythroid 2-related factor 2 (Nrf2).1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bollong, M.J., Yun, H., Sherwood, L., et al. A small molecule inhibits deregulated NRF2 transcriptional activity in cancer. ACS Chem. Biol. 10(10), 2193-2198 (2015).