Selective, reversible DNA-dependent protein kinase and mTOR inhibitor
Selective, reversible DNA-dependent protein kinase and mTOR inhibitor (IC50 values are 0.28 and 5.3 μM respectively). No affinity for PI3K, ATM and ATR (IC50 values are >100 μM). Able to induce apoptosis in vitro. Cell-permeable.
Store at Room Temperature. The product can be stored for up to 12 months.
Soluble in DMSO to 10 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Ballou LM et al. Inhibition of mammalian target of rapamycin signaling by 2-(morpholin-1-yl)pyrimido[2,1-alpha]isoquinolin-4-one. J Biol Chem282:24463-70 (2007).
Read more (PubMed: 17562705) »
Griffin RJ 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 Chem48:569-85 (2005).
Read more (PubMed: 15658870) »