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Compound 401

Cat No. 3271

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Chemical Name: 2-(4-Morpholinyl)-4H-pyrimido[2,1-a]isoquinolin-4-one

Biological Activity

Reversible and selective inhibitor of DNA-dependent protein kinase (DNA-PK) and mammalian target of rapamycin (mTOR) (IC₅₀ values are 0.28 and 5.3 μM respectively). Displays little affinity for other commonly studied kinases including PI 3-K, ATM and ATR (IC₅₀ values are all > 100 μM). Induces apoptosis in vitro.

Technical Data

M.Wt:

281.31

Formula:

C₁₆H₁₅N₃O₂

Solubility:

Soluble to 10 mM in DMSO and to 5 mM in ethanol

Purity:

>99 %

Storage:

Store at RT

CAS No:

[168425-64-7]

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis and MSDS.

Resources

Certificate of Analysis / MSDS

Certificate of Analysis: View current batch

Material Safety Data Sheet: View current batch

References

Griffen et al (2005) Selective benzopyranone and pyrimido[2,1-α]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. 48 569. Ballo et al (2007) Inhibition of mammalian target of rapamycin signaling by 2-(morpholin-1-yl)oyrimido[2,1-α]isoquinolin-4-one. J.Biol.Chem. 282 24463.

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Keywords: Compound 401, Selective, DNA-PK, mTOR, inhibitors, Wee1, Checkpoint, Control, Kinases, DNA-Dependent, Protein, Kinase, PI3K, Phosphoinositide, PI, 3-kinase, Akt, Signaling, Signalling, Mammalian, Target, Rapamycin, FRAP, Compound401