An inhibitor of Nrf2
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Nrf2-IN-1

Item No. 46392

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-(4-chlorophenyl)-1-[[4-(1,1-dimethylethyl)phenyl]methyl]-N-hydroxy-1H-pyrazole-5-carboxamide
CAS Number
1610022-76-8
Synonyms
  • Nrf2 Inhibitor 1
  • Nuclear Factor Erythroid 2-related factor 2-IN-1
  • Nuclear Factor Erythroid 2-related factor 2 Inhibitor 1
Molecular Formula
C21H22ClN3O2
Formula Weight
383.9
Purity
≥98%
Formulation (Request formulation change)
A solid
SMILES
O=C(NO)C1=CC(C2=CC=C(C=C2)Cl)=NN1CC(C=C3)=CC=C3C(C)(C)C
InChi Code
InChI=1S/C21H22ClN3O2/c1-21(2,3)16-8-4-14(5-9-16)13-25-19(20(26)24-27)12-18(23-25)15-6-10-17(22)11-7-15/h4-12,27H,13H2,1-3H3,(H,24,26)
InChi Key
ZFDMUUNGVLREEC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $175

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    10 mg

    $245

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    25 mg

    $350

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    50 mg

    $613

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    Cayman Chemical
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    Product Description

    Nrf2-IN-1 is an inhibitor of nuclear factor erythroid 2-related factor 2 (Nrf2).1 It inhibits Nrf2 transcriptional activity in a reporter assay using HeLa cells at 5 and 10 µM and reduces the expression of the Nrf2 target genes heme oxygenase-1 (HO-1) and glutamate-cysteine ligase modifier subunit (GCLM) in the same cells. Nrf2-IN-1 (10 µM) reduces Nrf2 protein levels in THP-1, HL-60, and U937 leukemia cells. It also reduces the growth of THP-1, HL-60, and U937 cells (IC50s = 5.33, 8.94, and 8.98 µM, respectively) and induces apoptosis in the same cells. Nrf2-IN-1 inhibits angiogenesis in a chorioallantoic membrane (CAM) assay.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zhang, J., Su, L., Ye, Q., et al. Discovery of a novel Nrf2 inhibitor that induces apoptosis of human acute myeloid leukemia cells. Oncotarget 8(5), 7625-7636 (2017).