A dual inhibitor of NOX1 and NOX4
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

GKT136901

Item No. 34205

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-(2-chlorophenyl)-4-methyl-5-(2-pyridinylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
CAS Number
955272-06-7
Synonyms
  • NOX Inhibitor IV
Molecular Formula
C19H15ClN4O2
Formula Weight
366.8
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:6): 0.14 mg/mlEthanol: 1 mg/ml
λmax
214, 257 nm
SMILES
O=C1C=C2NN(C3=C(Cl)C=CC=C3)C(C2=C(C)N1CC4=CC=CC=N4)=O
InChi Code
InChI=1S/C19H15ClN4O2/c1-12-18-15(10-17(25)23(12)11-13-6-4-5-9-21-13)22-24(19(18)26)16-8-3-2-7-14(16)20/h2-10,22H,11H2,1H3
InChi Key
DNKYHHFCPXKFIY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    5 mg

    $70

    Add

    10 mg

    $108

    Add

    25 mg

    $186

    Add

    50 mg

    $303

    Add
    Product Description

    GKT136901 is a dual inhibitor of NADPH oxidase 1 (NOX1) and NOX4 (Kis = 160 and 165 nM, respectively).1 It is selective for NOX1 and NOX4 over NOX2 and xanthine oxidase (Kis = 1,530 and >30,000 nM, respectively), as well as over a panel of 18 enzymes and ion channels at 10 µM. GKT136901 (0.1, 1, and 10 µM) scavenges peroxynitrite radicals, as well as prevents the nitration and dimerization of α-synuclein, in cell-free assays.2 It prevents peroxynitrite-induced cell death of differentiated LUHMES cells when used at a concentration of 10 µM.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Laleu, B., Gaggini, F., Orchard, M., et al. First in class, potent, and orally bioavailable NADPH oxidase isoform 4 (Nox4) inhibitors for the treatment of idiopathic pulmonary fibrosis. J. Med. Chem. 53(21), 7715-7730 (2010).

    2. Schildknecht, S., Weber, A., Gerding, H.R., et al. The NOX1/4 inhibitor GKT136901 as selective and direct scavenger of peroxynitrite. Curr. Med. Chem. 21(3), 365-376 (2014).