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ATM/ATR Inhibitors | Activators (14)


Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1009 BEZ235 (NVP-BEZ235, Dactolisib) BEZ235 (NVP-BEZ235, Dactolisib) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell.
  • Nature, 2012, 487(7408):505-9
  • Nat Med, 2015, 10.1038/nm.3855
  • Cancer Cell, 2012, 21(2):155-67
S1092 KU-55933 (ATM Kinase Inhibitor) KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor with IC50/Ki of 12.9 nM/2.2 nM in cell-free assays, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR.
  • Nature, 2015, 528(7582):422-6
  • Nature, 2015, 10.1038/nature14328
  • Science, 2016, 352(6283):353-8
S1570 KU-60019 KU-60019 is an improved analogue of KU-55933, with IC50 of 6.3 nM for ATM in cell-free assays, 270- and 1600-fold more selective for ATM than DNA-PK and ATR,and is a highly effective radiosensitizer.
  • Int J Cancer, 2015, 136(6):1445-57
  • Int J Cancer, 2013, 135(2):479-91
  • Biochem Pharmacol, 2013, 86(12):1708-20
S8007 VE-821 VE-821 is a potent and selective ATP competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM in cell-free assays, shows inhibition of H2AX phosphorylation, minimal activity against PIKKs ATM, DNA-PK, mTOR and PI3Kγ.
  • Nature, 2015, 518(7538):254-7
  • J Exp Med, 2013, 210(12):2675-92
  • Nat Commun, 2016, 10.1038/ncomms10660
S2758 Wortmannin Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Also blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays.
  • Nature, 2015, 10.1038/nature14412
  • Cancer Res, 2014, 74(10):2846-56
  • Cell Rep, 2015, 10.1016/j.celrep.2015.01.014
S7693 AZD6738 AZD6738 is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2.
S2245 CP-466722 CP-466722 is a potent and reversible ATM inhibitor, does not affect ATR and inhibits PI3K or PIKK family members in cells.
  • PLoS One, 2012, 7(11):e50423
  • J Neurooncol, 2012, 110(3):349-57
S2817 Torin 2 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 with EC50 of 28 nM/35 nM/118 nM,in PC3 cell lines respectively.
  • J Clin Invest, 2013, 124(2):742-54
  • Cell Rep, 2015, 11(3):446-59
  • Oncotarget, 2014, 5(20):10034-47
S8050 ETP-46464 ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.
S7136 CGK 733 CGK 733 is a potent and selective inhibitor of ATM/ATR with IC50 of ~200 nM.
S7050 AZ20 AZ20 is a novel potent and selective inhibitor of ATR kinase with IC50 of 5 nM in a cell-free assay, 8-fold selectivity over mTOR.
S7102 VE-822 VE-822 is an ATR inhibitor with IC50 of 19 nM in HT29 cells.
  • Sci Rep, 2016, 6:27379
  • J Virol, 2015, 10.1128/JVI.00389-15
S3600 Schisandrin B (Sch B) Schisandrin B is the most abundant dibenzocyclooctadiene lignan present in the traditional Chinese medicinal herb Schisandra chinensis (Turcz.) Baill.
S4157 Chloroquine Phosphate Chloroquine phosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator.
  • Sci Rep, 2016, 10.1038/srep23056.

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S1009 BEZ235 (NVP-BEZ235, Dactolisib) <1 mg/mL 0.01 mg/mL <1 mg/mL
S1092 KU-55933 (ATM Kinase Inhibitor) <1 mg/mL 33 mg/mL <1 mg/mL
S1570 KU-60019 <1 mg/mL 18 mg/mL <1 mg/mL
S8007 VE-821 <1 mg/mL 74 mg/mL <1 mg/mL
S2758 Wortmannin <1 mg/mL 85 mg/mL <1 mg/mL
S7693 AZD6738 <1 mg/mL 82 mg/mL 41 mg/mL
S2245 CP-466722 <1 mg/mL 0.28 mg/mL <1 mg/mL
S2817 Torin 2 <1 mg/mL 20 mg/mL <1 mg/mL
S8050 ETP-46464 <1 mg/mL 6 mg/mL <1 mg/mL
S7136 CGK 733 <1 mg/mL 100 mg/mL <1 mg/mL
S7050 AZ20 <1 mg/mL 83 mg/mL 3 mg/mL
S7102 VE-822 <1 mg/mL 36 mg/mL <1 mg/mL
S3600 Schisandrin B (Sch B) <1 mg/mL 80 mg/mL 10 mg/mL
S4157 Chloroquine Phosphate 100 mg/mL <1 mg/mL <1 mg/mL
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