A dual inhibitor of mTOR and DNA-PK (IC50s = 0.28 and 5.3 µM

Compound 401 – 5 mg

Brand:
Cayman
CAS:
168425-64-7
Storage:
-20
UN-No:
Non-Hazardous - /

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).{42995} 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.{42996} 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.  

 

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Description

A dual inhibitor of mTOR and DNA-PK (IC50s = 0.28 and 5.3 µM, respectively); selective for DNA-PK and mTOR over PI3K, ATM, and ATR (IC50s = >100 µM for all); inhibits phosphorylation of the mTOR targets S6K1 and Akt in Rat-1 fibroblasts and in M059J glioma cells that lack DNA-PK at 10 µM; inhibits proliferation of TSC1-/- MEFs (IC50 = 2 µM) but not TSC1+/+ MEFs; induces apoptosis in TSC1-/- MEFs

Formal name: 2-(4-morpholinyl)-4H-pyrimido[2,1-a]isoquinolin-4-one

Synonyms: 

Molecular weight: 281.3

CAS: 168425-64-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|DNA-PK||Product Type|Biochemicals|Kinase Inhibitors|mTOR||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|DNA-PK Signaling||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling

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