NU7026 is a potent DNA-PK inhibitor with IC50 of 0.23 μM in cell-free assays, 60-fold selective for DNA-PK than PI3K and inactive against both ATM and ATR.
LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM in cell-free assays, respectively more stable in solution than Wortmannin, and also blocks autophagosome formation.
Compound 401 is a synthetic inhibitor of DNA-PK and mTOR (IC50=5.3 μM). It has no inhibition on p110α/p85α PI3K (>100 μM) and blocks the phosphorylation of S6 kinase 1 Thr389 and Akt Ser473 in COS7 cells.
PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM.
PI-103 Hydrochloride is a dualPI3K and mTORinhibitor with IC50s of 8nM, 88nM, 48nM, 150nM, 20nM, and 83nM forp110α,p110β,p110δ,p110γ,mTORC1, and mTORC2. PI-103 Hydrochloride also inhibits DNA-PKwith a...
PIK-75 HCl is a p110α inhibitor with IC50 of 5.8 nM (200-fold more potently than p110β), isoform-specific mutants at Ser773, and also potently inhibits DNA-PK with IC50 of 2 nM in cell-free assays.
NU7441 (KU-57788) is a highly potent and selective DNA-PK inhibitor with IC50 of 14 nM and also inhibits PI3K with IC50 of 5 μM in cell-free assays.
PIK-90 is a DNA-PK and PI3Kinhibitor, which inhibitsp110α,p110γ and DNA-PKwith IC50s of 11, 18 and 13nM, respectively.
SF2523 is a highly selective and potent inhibitor of PI3K with IC50 values of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM in p53?/? MEFs cell line 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties. Inhibition of ATM/ATR/DNA-PK...
CC-115 is a dual inhibitor of DNA-dependent protein kinase (DNA-PK) and mammalian target of rapamycin (mTOR) with IC50 values of 0.013 μM and 0.021 μM, respectively. It has potential antineoplastic activity.
CC-115 hydrochloride is a potent and dualDNA-PK and mTORkinase inhibitor with IC50s of 13nM and 21nM, respectively. CC-115 blocks bothmTORC1 and mTORC2signaling.
STL127705 (Compound L) is aKu 70/80 heterodimer proteininhibitor, inhibits Ku70/80-DNA interaction, with an IC50 of 3.5μM. STL127705 also inhibits Ku-dependent activation of DNA-PKCS kinase (IC50, 2.5μM).
Nedisertib (M3814) is a potent, orally available and selective inhibitor of DNA-PK, with an IC50 of <3nM. Anti-tumor activity .
LTURM34 is a specific DNA-PK inhibitor, 170-fold more selective for DNA-PK activity compared to PI3K activity, with IC50 value of 0.034 μM.
YU238259 is a novel inhibitor of homology-dependent DNA repair(HDR), but does not inhibit non-homologous end-joining (NHEJ), in cell-based GFP reporter assays.
AZD7648 is a potent inhibitor of DNA-PK with an IC50 of 0.6 nM in biochemical assay and more than 100-fold selective against 396 other kinases.
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