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.
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 281.31. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.1 mM||35.55 mL||177.74 mL||355.48 mL|
|0.5 mM||7.11 mL||35.55 mL||71.1 mL|
|1 mM||3.55 mL||17.77 mL||35.55 mL|
|5 mM||0.71 mL||3.55 mL||7.11 mL|
References are publications that support the biological activity of the product.
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 PMID: 15658870
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 PMID: 17562705
If you know of a relevant reference for Compound 401, please let us know.
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Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.