A dual inhibitor of mTOR and DNA-PK
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.

Compound 401

Item No. 21769

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-(4-morpholinyl)-4H-pyrimido[2,1-a]isoquinolin-4-one
CAS Number
168425-64-7
Molecular Formula
C16H15N3O2
Formula Weight
281.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 1 mg/mlEthanol: 0.5 mg/ml
λmax
214, 252, 276 nm
SMILES
O=C1N2C(C(C=CC=C3)=C3C=C2)=NC(N4CCOCC4)=C1
InChi Code
InChI=1S/C16H15N3O2/c20-15-11-14(18-7-9-21-10-8-18)17-16-13-4-2-1-3-12(13)5-6-19(15)16/h1-6,11H,7-10H2
InChi Key
BVRDQVRQVGRNHG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice 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

    1 mg

    $36

    Add

    5 mg

    $128

    Add

    10 mg

    $169

    Add

    25 mg

    $378

    Add
    Kinase Resource Center
    Discover Products & Resources for Kinase Research
    • Kinase inhibitors, screening libraries, assay kits, & more
    • Tools to study kinase signaling pathways:
      • Growth factor signaling
      • PI3K/Akt/mTOR
      • MAPKs (ERK, p38, & JNK)
      • JAK/STAT signaling
    • Articles, resources, & advice
    EXPLORE NOW
    Product Description

    Compound 401 is an inhibitor of DNA-dependent protein kinase (DNA-PK) and mammalian target of rapamycin (mTOR; IC50s = 0.28 and 5.3 µM, respectively).1 It is selective for DNA-PK and mTOR over PI3K, ATM, and ATR (IC50s = >100 µM for all). Compound 401 (10 µM) inhibits phosphorylation of the mTOR targets S6K1 and Akt in Rat-1 fibroblasts and in M059J glioma cells that lack DNA-PK.2 It inhibits proliferation of mouse embryonic fibroblasts (MEFs) lacking tuberous sclerosis complex 1 (TSC1-/-; IC50 = 2 µM), a complex associated with hamartomas that display hyperactive mTOR signaling, but not TSC1+/+ MEFs. Compound 401 also induces apoptosis in TSC1-/- MEFs.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Griffin, R.J., Fontana, G., Golding, B.T., et al. Selective benzopyranone and pyrimido[2,1-a]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: Synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in vitro. J. Med. Chem. 48(2), 569-585 (2005).

    2. Ballou, L.M., Selinger, E.S., Choi, J.Y., et al. Inhibition of mammalian target of rapamycin signaling by 2-(morpholin-1-yl)pyrimido[2,1-α]isoquinolin-4-one. The Journal of Biological Chemisty 282(33), 24463-24470 (2007).