Signaling Pathway

ATM/ATR

ATM/ATR

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ATM/ATR are members of the PI-3 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.

ATM/ATR Inhibitors & Modulators (12)

Product Name Catalog No. Brief Description
AZ20

HY-15557

AZ20 is a potent and selective inhibitor of ATR with an IC50 of 5 nM; 8-fold selectivity over mTOR(IC50=38 nM).

AZD0156

HY-100016

AZD0156 is an oral, potent and selective ATM kinase inhibitor, inhibiting the kinase activity of ATM and ATM-mediated signaling, preventing DNA damage checkpoint activation, and disrupting DNA damage repair, inducing tumor cell apoptosis, and leading to cell death in ATM-overexpressing tumor cells.

AZD6738

HY-19323

AZD6738 is a potent inhibitor of ATR kinase activity with an IC50 of 1 nM against the isolated enzyme and 74 nM against ATR kinase-dependent CHK1 phosphorylation in cells.

CGK733

HY-15520

CGK 733 is a small molecule inhibitor reportedly targeting the kinase activities of ATM and ATR.

CP-466722

HY-11002

CP-466722 is rapidly reversible potential ATM kinase inhibitor.

ETP-46464

HY-15521

ETP-46464 is a cell-permeable quinoline-containing heterotricyclic compound that acts as a potent inhibitor against mTOR, ATR, DNA-PK, PI 3-Kα, and ATM (IC50= 0.6, 14, 36, 170, and 545 nM, respectively).

HLM006474

HY-16667

HLM006474 is a potent inhibitor of melanocytes proliferation and subsequent invasion in a three-dimensional tissue culture model system; interferes with E2F activity.

KU-55933

HY-12016

KU-55933 is a potent ATM inhibitor with an IC50 and Ki of 13 and 2.2 nM, respectively; highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR.

KU-60019

HY-12061

KU-60019 is an improved analogue of KU-55933, with IC50 of 6.3 nM for ATM.

VE-821

HY-14731

VE-821 is a potent and selective ATP competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM.

VE-822

HY-13902

VE-822 is a selective ATR inhibitor with an Ki value of 0.2 nM, >150 fold selectivity over ATM (Ki=34 nM), DNA-PK (Ki >4 uM) and mTOR (Ki >1 uM).

Wortmannin

HY-10197

Wortmannin is a multi-target inhibitor of PI3K and MLCK with IC50 of 3 nM and 0.17 μM, respectively.