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    ATM/ATR

    ATM/ATR are members of the PI3 family of serine-threonine kinases and function as essential links between the sensors and effectors of the DNA damage response. The roles of ATM and ATR partially overlap and are cooperative; however they are also known to play distinct roles in protecting the cell from DNA damage. ATM is mostly responsible for sending signals from DSBs (double-strand breaks) induced by ionizing radiation while the closely related ATR responds to UV damage or stalled replication forks. ATM and ATR are known to phosphorylate common as well as specific substrates to activate checkpoint signaling. The G1, S, and G2 cell cycle checkpoints are primarily regulated by the ATM (ataxia telangiectasia, mutated) and ATR (ATM and Rad3-related) protein kinases.

    Products

    Catalog No. Name Description
    GY01751 Special CP-466722 CP-466722 is a rapidly reversible inhibitor of ATM, with an IC50 of 4.1 μM, and has no effects on PI3K or closely related PI3K-like protein kinase (PIKK) family members.
    GY01063 Special KU-55933 KU-55933 is a potent ATM inhibitor with an IC50 and Ki of 12.9 and 2.2 nM, respectively, and highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR.
    GY01100 Special VE-821 VE-821 is a potent ATP-competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM.
    GY01198 Special VE-822 (Berzosertib) VE-822 is an ATR inhibitor with Ki value of <0.2 nM, also inhibits ATM with Ki of 34 nM.
    GY04008 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.
    GY01694 ETP-46464 ETP-46464 is an effective mTOR and ATR inhibitor with IC50s of 0.6 and 14 nM, respectively.
    GY01983 BAY-1895344 HCl BAY-1895344 hydrochloride is a potent, orally available and selective ATR inhibitor, with IC50 of 7 nM.
    GY01151 AZD6738 AZD6738 is a potent inhibitor of ATR kinase with an IC50 of 1 nM.
    GY04482 BAY 1895344 BAY 1895344 is a potent, highly selective and orally available ATR inhibitor with an IC50 of 7 nM.
    GY05055 GSK 635416A GSK 635416A is a novel ATM inhibitor with highly selective radiosensitizing activity, inhibits radiation induced phosphorylation of ATM.
    GY05106 CBP-93872 A potent G2 checkpoint inhibitor that specifically abrogates the DNA double-stranded break (DSB)-induced G2 checkpoint.
    GY05628 AZ32 AZ32 (ATM inhibitor AZ32) is a potent, selective, orally bioavailable, BBB-penetrating ATM inhibitor with IC50 of <6.2 nM, effectively blocks ATM auto-phosphorylation at S1981 with IC50 of 0.31 uM.