ATM / ATR

Inhibitory Selectivity

Catalog No.	Inhibitor Name	ATM	ATR	Other Targets
A10133	Dactolisib		***	p110α,p110γ,mTOR (p70S6K)
A10506	KU-55933	****		DNA-PK,mTOR,PI3K
A10507	KU-60019	****
A11605	VE-821		***
A11161	Wortmannin	**	*	PI3K,DNA-PK,MLCK
A11586	Torin 2	***	**	mTOR,DNA-PK
A11086	CP-466722	**
A13289	VE-822	*	***
A13328	ETP-46464	*	***	mTOR,DNA-PK,PI3Kα
A13191	CGK 733	**	**
A13205	AZ20		****	mTOR
A15794	AZD6738		****
A11991	Schisandrin B		*

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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KU 59403

Catalog No. A20928
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ATM inhibitor

KU 59403 is a potent ATM inhibitor, with an IC50 of 3 nM. 了解更多

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AZD1390

Catalog No. A16798
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ATM 抑制剂

AZD1390是一流的口服中枢神经渗透性ATM抑制剂，在细胞中的IC50为0.78 nM，对PIKK酶家族中密切相关的成员具有10,000倍以上的选择性，并且在多种激酶中均具有出色的选择性。了解更多

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AZ31

Catalog No. A16813
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ATM 抑制剂

AZ31是一种新的选择性ATM抑制剂，IC50<0.0012 uM，对密切相关的酶具有良好的选择性（对DNA-PK和PI3Kα的选择性大于500倍，对mTOR、PI3Kβ和PI3Kγ的选择性大于1000倍）。了解更多

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AZ32

Catalog No. A16814
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ATM 抑制剂

AZ32是ATM激酶的特异性抑制剂，对小鼠具有良好的BBB渗透性，ATM酶的IC50值<0.0062 uM。它对ATR有足够的选择性，并且具有较高的细胞通透性。了解更多

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NU6027

Catalog No. A14136
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ATR/CDK 抑制剂

NU6027是一种有效的细胞ATR活性抑制剂（IC（50）=6.7μM），并以ATR依赖的方式增强羟基脲和顺铂的细胞毒性。了解更多

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AZD0156

Catalog No. A16419
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ATM 抑制剂

AZD0156是有效且选择性的ATM激酶抑制剂，具有潜在的化学/放射致敏和抗肿瘤活性。了解更多

Product Citations (1)

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- Yi-Ru Pan, .et al. ATM Inhibitor Suppresses Gemcitabine-Resistant BTC Growth in a Polymerase θ Deficiency-Dependent Manner, Biomolecules, 2020, Nov 9;10(11):1529 PMID: 33182492
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Mirin

Catalog No. A15842
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ATM 抑制剂

Mirin可防止ATM激活以响应双链断裂（IC50 = 12 uM），并诱导G2细胞周期停滞。了解更多

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AZD6738 (Ceralasertib)

Catalog No. A15794
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ATR 抑制剂

AZD6738是一种有效的ATR激酶抑制剂，对分离的酶的IC50为1 nM，对细胞中ATR激酶依赖性CHK1磷酸化的IC50为74 nM。了解更多

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- Brian F Kiesel, .et al. Dose-dependent bioavailability and tissue distribution of the ATR inhibitor AZD6738 (ceralasertib) in mice, Cancer Chemother Pharmacol, 2022, Feb;89(2):231-242 PMID: 35066692
- Albert Job, .et al. The POLD1 R689W variant increases the sensitivity of colorectal cancer cells to ATR and CHK1 inhibitors, Sci Rep, 2020, Nov 3;10(1):18924 PMID: 33144657
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VE-822

Catalog No. A13289
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ATR 抑制剂

VE-822是有效的ATR抑制剂。了解更多

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ETP-46464

Catalog No. A13328
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ATR 抑制剂

ETP-46464是一种有效的选择性ATR抑制剂，IC50为25 nM。了解更多

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- Fu-Xing Gong, .et al. De-dimerization of PTB is catalyzed by PDI and is involved in the regulation of p53 translation, Nucleic Acids Res, 2021, Sep 20;49(16):9342-9352 PMID: 34403458
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AZ-20

Catalog No. A13205
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ATR kinase 抑制剂

AZ20是一种有效的选择性ATR抑制剂，IC50值为5 nM。了解更多

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CGK 733

Catalog No. A13191
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ATM/ATR 抑制剂

CGK733是ATR和ATM激酶的选择性抑制剂。在过早衰老的乳腺癌细胞中诱导细胞死亡。了解更多

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Torin 2

Catalog No. A11586
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mTOR 抑制剂

Torin 2 是有效的选择性mTOR抑制剂 (IC50 = 2.1 nM)。在PI3K上显示mTOR的800倍细胞选择性（mTOR和PI3K的细胞EC50值分别为0.25和200 nM）。了解更多

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- Diane Yang, .et al. Pancreatic Differentiation of Stem Cells Reveals Pathogenesis of a Syndrome of Ketosis-Prone Diabetes, Diabetes, 2021, Oct;70(10):2419-2429 PMID: 34344789
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VE-821

Catalog No. A11605
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ATM/ATR 抑制剂

VE-821是一种有效且选择性的蛋白激酶ATR抑制剂。了解更多

Product Citations (5)

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- Mitsuru Sasaki-Honda, .et al. A patient-derived iPSC model revealed oxidative stress increases facioscapulohumeral muscular dystrophy-causative DUX4, Hum Mol Genet, 2018, Dec 1; 27(23): 4024-4035 PMID: 30107443
- Kim J, .et al. Replication Stress Shapes a Protective Chromatin Environment across Fragile Genomic Regions, Mol Cell, 2018, Jan 4;69(1):36-47.e7 PMID: 29249653
- Antonio Postigo, .et al. Cytoplasmic ATR Activation Promotes Vaccinia Virus Genome Replication, Cell Rep, 2017, May 2; 19(5): 1022-1032 PMID: 28467896
- Nnennaya Kanu, .et al. DNA replication stress mediates APOBEC3 family mutagenesis in breast cancer, Genome Biol, 2016, 17: 185 PMID: 27634334
- Carolyn Botting, .et al. H2AX phosphorylation and DNA damage kinase activity are dispensable for herpes simplex virus replication, Virol J, 2016, 13: 15 PMID: 26817608
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KU-60019

Catalog No. A10507
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ATM 抑制剂

KU-60019是一种强效特异性ATM抑制剂，IC50为6.3 nM。了解更多

Product Citations (4)

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- Fu-Xing Gong, .et al. De-dimerization of PTB is catalyzed by PDI and is involved in the regulation of p53 translation, Nucleic Acids Res, 2021, Sep 20;49(16):9342-9352 PMID: 34403458
- Hegedus C, .et al. PARP1 Inhibition Augments UVB-Mediated Mitochondrial Changes-Implications for UV-Induced DNA Repair and Photocarcinogenesis, Cancers (Basel), 2019, Dec 18;12(1) PMID: 31861350
- Masaya Igase, .et al. Combination Therapy with Reovirus and ATM Inhibitor Enhances Cell Death and Virus Replication in Canine Melanoma, Mol Ther Oncolytics, 2019, vol 15 PMID: 31650025
- CHENGHUA LOU, .et al. Targeting the ataxia telangiectasia mutated pathway for effective therapy against hirsutine-resistant breast cancer cells, Oncol Lett, 2016, Jul; 12(1): 295-300 PMID: 27347141
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Wortmannin

Catalog No. A11161
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PI3K 抑制剂

Wortmannin是一种有效的，选择性的，可透过细胞的且不可逆的磷脂酰肌醇3-激酶（PI 3-激酶）（IC50 = 2-4 nM）抑制剂，它也有效抑制polo-like激酶1（PLK1）（IC50 = 5.8 nM）。了解更多

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- Dongdong Fang, etc. Epithelial-Mesenchymal Transition of Ovarian Cancer Cells Is Sustained by Rac1 through Simultaneous Activation of MEK1/2 and Src Signaling Pathways. Oncogene. 2017 Mar; 36(11): 1546–1558.
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CP-466722

Catalog No. A11086
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ATM 抑制剂

CP-466722是一种特殊的ATM抑制剂，可抑制细胞依赖ATM的磷酸化事件，并且ATM功能的破坏会导致特征性的细胞周期检查点缺陷。了解更多

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KU-55933

Catalog No. A10506
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ATM 抑制剂

KU-55933是ATM抑制剂，通过抑制细胞增殖，并通过阻断Akt过度激活的癌细胞中的Akt诱导凋亡。了解更多

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- Mariko Shikata, .et al. 4-(Methylnitrosamino)-1-(3-pyridyl)-1-butanone-Induced Histone Acetylation via α7nAChR-Mediated PI3K/Akt Activation and Its Impact on γ-H2AX Generation, Chem Res Toxicol, 2021, Dec 20;34(12):2512-2521 PMID: 34784199
- Masaya Igase, .et al. Combination Therapy with Reovirus and ATM Inhibitor Enhances Cell Death and Virus Replication in Canine Melanoma, Mol Ther Oncolytics, 2019, vol 15 PMID: 31650025
- Hayakawa K, .et al. Planar compression of extracellular substrates induces S phase arrest via ATM-independent CHK2 activation, Biochem Biophys Res Commun, 2018, Dec 2;506(4):983-989 PMID: 30404732
- Chwastek J, .et al. The ATM kinase inhibitor KU-55933 provides neuroprotection against hydrogen peroxide-induced cell damage via a γH2AX/p-p53/caspase-3-independent mechanism: Inhibition of calpain and cathepsin D, Int J Biochem Cell Biol, 2017, Jun;87:38-53 PMID: 28341201
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BEZ235 (NVP-BEZ235, Dactolisib)

Catalog No. A10133
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PI3K/mTOR 抑制剂

BEZ235 (NVP-BEZ235,Dactolisib)是通过与这些酶的ATP结合裂隙结合来抑制PI3K和mTOR激酶活性。了解更多

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- Makoto Koyama, .et al. Low-dose trametinib and Bcl-xL antagonist have a specific antitumor effect in KRAS-mutated colorectal cancer cells, Int J Oncol, 2020, Sep 2 PMID: 32901840
- Tzeng SF, .et al. O-Glycosylation-mediated signaling circuit drives metastatic castration-resistant prostate cancer, FASEB J, 2018, Jun 15:fj201800687 PMID: 29906246
- Dominik Schulz, .et al. HNSCC cells resistant to EGFR pathway inhibitors are hypermutated and sensitive to DNA damaging substances, Am J Cancer Res, 2016, 6(9): 1963-1975 PMID: 27725902