dna-pk

LY294002 (SF 1101) is a broad-spectrum inhibitor of PI3K, inhibiting PI3Kα, PI3Kδ, and PI3Kβ (IC50=0.5 0.57 0.97 μM). LY294002 is also an inhibitor of DNA-PK (IC50=1.4 μM) and an inhibitor of CK2 (IC50=98 nM). LY294002 activates apoptosis and autophagy.

Torin 1 is an effective inhibitor of mTORC1 2 with (IC50: 2 nM 10 nM); has 1000-fold selectivity for mTOR than PI3K.

Wortmannin (SL-2052) is a PI3K inhibitor (IC50=3 nM) that is covalent and irreversible. Wortmannin is also an inhibitor of PlK1 and PlK3 (IC50=5.8 48 nM) that blocks autophagy.

OSI-027 (ASP4786) is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, and more than 100-fold selectivity observed for mTOR than PI3Kα, PI3Kβ, PI3Kγ or DNA-PK. Phase 1.

NU7441 (KU-57788 (NU7441)) is a highly effective and specific DNA-PK inhibitor (IC50: 14 nM).

PIK-75, a DNA-PK and PI3K inhibitor, suppresses DNA-PK(IC50=2 nM), p110α(IC50=5.8 nM) and p110γ(IC50=76 nM).

ETP-46464 is an effective and specific ATR inhibitor (IC50: 25 nM).

KU-55933 (ATM Kinase Inhibitor) is an ATM inhibitor (IC50=12.9 nM; Ki=2.2 nM) that is selective and ATP-competitive. KU-55933 induces apoptosis and has antitumor effects.

Torin 2(IC50=0.25 nM), a specific and effective mTOR inhibitor, is the 800-fold greater specific activity for mTOR than PI3K and improves pharmacokinetic properties. The EC50 of Torin 2 for ATM ATR DNA-PK inhibition is 28 nM 35 nM 118 nM, respectively.

KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 values of 8.6 nM, 4 nM, 0.5 nM, and 0.1 nM respectively, and demonstrates less inhibition of PI3Kγ with an IC50 of 0.59 μM.

PI-3065 is a novel potent and selective PI3K p110δ inhibitor.

PIK-90, a DNA-PK and PI3K inhibitor, suppresses p110α( IC50=11 nM), p110γ(IC50=18 nM) and DNA-PK(IC50=13 nM) .

Voxtalisib (XL765) (SAR245409, XL765) is a dual inhibitor of mTOR PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1 2.

DNA-PK-IN-15 (compound 6) acts as an inhibitor of DNA-PK, exhibiting an IC50 value of 0.08 nM.

AZD 6482 (KIN-193) is a potent and selective inhibitor of p110β and PI3Kβ with IC50 values ​​of 0.69nM and 10nM, respectively. AZD 6482 is particularly effective in blocking AKT signaling and tumor growth dependent on p110β activation or PTEN loss.

CC-115 is a inhibitor of mTOR DNA-PK (IC50= 21 13 nM).

PI-103 is a potent, cell-permeable, ATP-competitive inhibitor of PI3K family members (IC50s: 2 3 3 15 30 23 nM for p110α β δ γ, mTOR, and DNA-PK).

AZD-7648 is an inhibitor of DNA-dependent protein kinase (DNA-PK) with the IC50 of 0.63 nM in an enzyme assay,has anti-tumor activity.

DNA-PK-IN-10 is a DNA-PK inhibitor used in breast cancer and non-small cell lung cancer research [1].

NU 7026 (DNA-PK Inhibitor II) is an effective DNA-PK inhibitor (IC50: 0.23 μM, in cell-free assays), 60-fold selective for DNA-PK than PI3K and no inhibition against both ATM and ATR.

Onatasertib (CC223) is an orally available mTOR inhibitor with potential antitumor activity. Onatasertib inhibits the activity of mTOR, which may result in the induction of tumor cell apoptosis and a decrease in tumor cell proliferation. Onatasertib is a potent mTOR kinase inhibitor (IC50: 16 nM), with >150-fold sensitivity than the related lipid kinase PI3Kα (IC50: 4 μM).

Compound 401 (2-morpholino-4H-pyrimido[2,1-a]isoquinolin-4-one) is a synthetic DNA-PK inhibitor (IC50 = 0.28 μM) that also targets mTOR but not PI3K.

PIK-93, the first potent synthetic PI4K inhibitor, exhibits an IC50 of 19 nM and also inhibits PI3Kα with an IC50 of 39 nM.

PIK-75 hydrochloride (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.