Cayman Compound 401

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.