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ATM/ATR

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.

Ataxia telangiectasia mutated (11)
产品名称 目录号 简述
AZ20 HY-15557

AZ20是高活性ATR抑制剂,IC50为5 nM,对mTOR的IC50为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

CGK733是ATM/ATR选择性抑制剂,IC50为200 nM。

CP-466722 HY-11002

CP-466722是快速可逆的ATM激酶抑制剂。

ETP-46464 HY-15521

ETP-46464是可渗透入细胞的多靶点抑制剂,对mTOR,ATR,DNA-PK,PI3-Kα和ATM的IC50分别为0.6,14,36,170和545 nM。

KU-55933 HY-12016

KU-55933是ATM抑制剂,IC50和Ki分别为13和2.2 nM,对DNA-PK,PI3K/PI4K,ATR和mTOR的活性较低。

KU-60019 HY-12061

KU-60019是KU-55933的改良类似物,对ATM的IC50为6.3 nM。

VE-821 HY-14731

VE-821是ATP竞争性,高活性ATR选择性抑制剂,Ki和IC50分别为13 nM和26 nM,与ATM,DNA-PK和mTOR等的交叉反应极低。

VE-822 HY-13902

VE-822是高亲和力ATR选择性抑制剂,Ki为0.2 nM,对ATM,DNA-PK和mTOR的Ki为34 nM,>4 uM和>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.

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