Pictilisib dimethanesulfonate is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold). |
(R)-(-)-Rolipram is the R-enantiomer of Rolipram. Rolipram is a selective inhibitor of phosphodiesterases PDE4(IC50 of 3 nM, 130 nM and 240 nM for PDE4A, PDE4B,...
LTURM34 is an inhibitor of DNA-PK with IC50 of 34 nM. LTURM34 displays effective antiproliferative activity in a wide range of tumor cell lines. LTURM34 shows 1...
LY-2940094 decreases ethanol self-administration in animal models. LY-2940094 is an effective, selective, and orally available nociceptin receptor antagonist wi...
Voxtalisib (SAR245409, XL765)Analogue is a dual inhibitor of mTOR/PI3K, mostly for p110γ , also inhibits DNA-PK and mTOR. |
LY294002 is an inhibitor of PI3K (IC50s: 0.5/0.57/0.97 μM for PI3Kα/δ/β in cell-free assays). It also blocks autophagosome formation. |
PI-3065 is a novel potent and selective PI3K p110δ inhibitor. |
ETP-46464 is an effective and specific ATR inhibitor (IC50: 25 nM). |
PIK-75 Hydrochloride is a p110α inhibitor with IC50 of 5.8 nM (200-fold more potently than p110β), isoform-specific mutants at Ser773, and also potently inhib...
XL147 analogue is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ. |
NU7026 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...
PIK-90, a DNA-PK and PI3K inhibitor, suppresses p110α( IC50=11 nM), p110γ(IC50=18 nM) and DNA-PK(IC50=13 nM) . |
PIK-93 is the first potent, synthetic PI4K inhibitor with IC50 of 19 nM; inhibits PI3Kα with IC50 of 39 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). |
KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor. |
CC-223 is an orally available mTOR inhibitor with potential antitumor activity. CC-223 inhibits the activity of mTOR, which may result in the induction of tumor...
CC-115 is a inhibitor of mTOR/DNA-PK (IC50= 21/ 13 nM). |
Compound 401 is a synthetic DNA-PK inhibitor (IC50 = 0.28 μM) that also targets mTOR but not PI3K. |
SF2523 is a highly selective and potent inhibitor. |
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. |
Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor (IC50: 11 nM). |
Torin 1 is an effective inhibitor of mTORC1/2 with (IC50: 2 nM/10 nM); has 1000-fold selectivity for mTOR than PI3K. |
AZD 6482 is a potent and selective p110β inhibitor with IC50 of 0.69 nM and a PI3Kβ inhibitor with IC50 of 10 nM. |
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 proper...
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). |
NU7441 (KU-57788) is a highly effective and specific DNA-PK inhibitor (IC50: 14 nM). |
Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM, with little selectivity within the PI3K family. Also blocks autophagosome formation and pote...
OSI-027 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 PI...
KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 of 8.6 nM and 4 nM, 0.5 nM, 0.1 nM respectively, less inhibition of PI3Kγ with IC...
NU6027 is a potent ATR/CDK inhibitor, inhibits CDK1/2, ATR and DNA-PK with Ki of 2.5 μM/1.3 μM, 0.4 μM and 2.2 μM, enter cells more readily than the 6-amino...
LY3023414 is an oral ATP competitive inhibitor of the class I PI3K isoforms, DNA-PK, and mTOR. LY3023414 has been used in trials studying the treatment of Neopl...
Voxtalisib (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. |
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. |