ATM/ATR

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ATM/ATR Inhibitors | Activators (14)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
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
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
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
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
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
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
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.
  • Cell Signal, 2016, 28(8):1086-98
S8050 ETP-46464 ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.
Cat.No. Product Name Information Product Use Citation Customer Product Validation
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.
  • Mol Oncol, 2016, 10(5):751-63
S3600 Schisandrin B (Sch B) Schisandrin B is the most abundant dibenzocyclooctadiene lignan present in the traditional Chinese medicinal herb Schisandra chinensis (Turcz.) Baill.
S7693 AZD6738 AZD6738 is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2.

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
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
S2245 CP-466722 <1 mg/mL 0.28 mg/mL <1 mg/mL
S7102 VE-822 <1 mg/mL 36 mg/mL <1 mg/mL
S1009 BEZ235 (NVP-BEZ235, Dactolisib) <1 mg/mL 0.01 mg/mL <1 mg/mL
S2758 Wortmannin <1 mg/mL 85 mg/mL <1 mg/mL
S2817 Torin 2 <1 mg/mL 20 mg/mL <1 mg/mL
S4157 Chloroquine Phosphate 100 mg/mL <1 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
S3600 Schisandrin B (Sch B) <1 mg/mL 80 mg/mL 10 mg/mL
S7693 AZD6738 <1 mg/mL 82 mg/mL 41 mg/mL
Tags: ATM inhibition | ATR inhibition | ATM kinase activation | ATM kinase assay | ATM protein kinase | ATM signaling pathway | ATM inhibitor drugs | ATM tumor | ATM phosphorylation | ATM targets | ATM cancer | ATM activity | ATM inhibitor clinical trial | ATM inhibitor review
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