An inhibitor of NOX2 and RNase H2
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NOX Inhibitor VII

Item No. 46371

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-fluoro-2-(2-methylphenyl)-1,2-benzisothiazol-3(2H)-one
CAS Number
727664-79-1
Synonyms
  • NADPH Oxidase Inhibitor VII
  • Thr101
Molecular Formula
C14H10FNOS
Formula Weight
259.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Chloroform: Sparingly Soluble: 1-10 mg/mlDMSO: Sparingly soluble: 1-10 mg/ml
SMILES
CC1=C(C=CC=C1)N(SC2=CC(F)=CC=C23)C3=O
InChi Code
InChI=1S/C14H10FNOS/c1-9-4-2-3-5-12(9)16-14(17)11-7-6-10(15)8-13(11)18-16/h2-8H,1H3
InChi Key
BUIZTXXZBDUOCR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $39

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    5 mg

    $137

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    10 mg

    $215

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    Cayman Chemical
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    Product Description

    NOX inhibitor VII is an inhibitor of NADPH oxidase 2 (NOX2; EC50 = 0.3 µM in PMA-stimulated neutrophils) and RNase H2 (IC50 = 0.01 µM).1,2 It is selective for NOX2 over NOX1, NOX4, and NOX5 (EC50s = 3, 8, and 8 µM, respectively, in cell-based assays) and for RNase H2 over RNase H1 (IC50 = 2 µM). However, NOX inhibitor VII also inhibits phosphomannose isomerase and several histone deacetylases (HDACs; IC50s = 2.9 and 0.66-6.07 µM, respectively) and, to a lesser extent, the tautomerase activity of macrophage migration inhibitory factor (MIF; IC50 = 62 µM).3,4,5 NOX inhibitor VII (2.5 µM) is selectively cytotoxic to MDA-MB-231 and BT-549 breast cancer cells over non-cancerous MCF-10A breast epithelial cells, and it induces apoptosis and DNA damage in MDA-MB-231 cells.6 It enhances programmed cell death protein 1 (PD-1) antibody-induced decreases in tumor volume and increases in intratumoral T cell infiltration in an immunocompetent syngeneic T11 murine model of triple-negative breast cancer (TNBC).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Smith, S.M., Min, J., Ganesh, T., et al. Ebselen and congeners inhibit NADPH oxidase 2-dependent superoxide generation by interrupting the binding of regulatory subunits. Chem. Biol. 19(6), 752-763 (2012).

    2. White, R., Saxty, B., Large, J., et al. Identification of small-molecule inhibitors of the ribonuclease H2 enzyme. J. Biomol. Screen. 18(5), 610-620 (2013).

    3. Dahl, R., Bravo, Y., Sharma, V., et al. Potent, selective, and orally available benzoisothiazolone phosphomannose isomerase inhibitors as probes for congenital disorder of glycosylation Ia. J. Med. Chem. 54(10), 3661-3668 (2011).

    4. Wang, Y., Wallach, J., Duane, S., et al. Developing selective histone deacetylases (HDACs) inhibitors through ebselen and analogs. Drug Des. Devel. Ther. 11, 1369-1382 (2017).

    5. Sumaiya, K., Selvambika, P., and Natarajaseenivasan, K. Anti-macrophage migration inhibitory factor (MIF) activity of ibudilast: A repurposing drug attenuates the pathophysiology of leptospirosis. Microb. Pathog. 173(Pt A), 105786 (2022).

    6. Nguyen, T.Q.A., Zhang, J., Dai, H., et al. Targeting RNase H2: A dual-mechanism strategy to elevate replication stress, DNA damage, and antitumor immunity in TNBC. Cell Rep. Med. 7(5), 102750 (2026).