DNA-PK

Inhibitory Selectivity

Catalog No.	Inhibitor Name	DNA-PK	Other
A10726	PI-103	**	p110α,p110δ,p110β
A11098	NU7441	***	mTOR,PI3K
A10729	PIK-75	****	p110α,p110γ,p110δ
A12752	NU7026	*	PI3K
A11207	PP121	**	PDGFR,Hck,VEGFR
A13224	KU-0060648	***	PI3Kδ,PI3Kβ,PI3Kα
A11778	Compound 401	*	mTOR,PI3K
A13328	ETP-46464	***	ATM, ATR, PI3Kα, mTOR
A15779	CC-115	***	mTOR

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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PI-103

Catalog No. A10726
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PI3K 抑制剂

PI-103是一种有效的，细胞可渗透的，ATP竞争性磷脂酰肌醇3激酶（PI3K）家族抑制剂，对DNA-PK，PI3K（p110α）和mTOR具有选择性。了解更多

Product Citations (2)

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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
- Byungki Jang, .et al. The Peptidylarginine Deiminase Inhibitor Cl-Amidine Suppresses Inducible Nitric Oxide Synthase Expression in Dendritic Cells, Int J Mol Sci, 2017, Nov; 18(11): 2258 PMID: 29077055
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NU-7441 (KU-57788)

Catalog No. A11098
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DNA-PK 抑制剂

NU-7441 (KU-57788)是一种有效的选择性DNA依赖性蛋白激酶（DNA-PK）抑制剂。对于DNA-PK，mTOR，PI 3-K，ATM和ATR，IC50值分别为14、1700、5000，> 100000和> 100000 nM。了解更多

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- Shahar Biechonski, .et al. Attenuated DNA damage responses and increased apoptosis characterize human hematopoietic stem cells exposed to irradiation, Sci Rep, 2018, Apr 17 PMID: 29666389
- Ihara M, .et al. Expression of the DNA-dependent protein kinase catalytic subunit is associated with the radiosensitivity of human thyroid cancer cell lines, J Radiat Res, 2018, Nov 23 PMID: 30476230
- 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
- Masaaki Yanai, .et al. DNA-PK Inhibition by NU7441 Enhances Chemosensitivity to Topoisomerase Inhibitor in Non-Small Cell Lung Carcinoma Cells by Blocking DNA Damage Repair, Yonago Acta Med, 2017, Mar; 60(1): 9-15 PMID: 28331416
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PP121

Catalog No. A11207
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PI3K 抑制剂

PP121是一种作用于PDGFR，Hck，mTOR，VEGFR2，Src和Abl的多靶点抑制剂，IC50分别为2 nM，8 nM，10 nM，12 nM，14 nM和18 nM，也抑制DNA-PK，IC50为60 nM。了解更多

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PIK-75 hydrochloride

Catalog No. A10729
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PI3K 抑制剂

PIK-75是一种p110α抑制剂，IC50值为5.8nM。在p110γ和p110β的效果较差，IC50值为0.076 ?M和1.3 ?M。了解更多

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- Pridham KJ, .et al. PIK3CB/p110β is a selective survival factor for glioblastoma, Neuro Oncol, 2018, Mar 27;20(4):494-505 PMID: 29016844
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Compound 401

Catalog No. A11778
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DNA-PK 抑制剂

Compound 401是一种细胞可渗透的嘧啶-异喹啉酮化合物，可作为有效的，可逆的和ATP竞争的DNA-PK抑制剂（IC50 = 280 nM），选择性是mTOR（IC50 = 5.3μM）的19倍。了解更多

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KU 0060648

Catalog No. A13224
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DNA-PK 抑制剂

KU0060648是一种有效且选择性的DNA依赖性蛋白激酶（DNA-PK）抑制剂（IC50 = 8.6 nM）；对DNA-PK的选择性是其他PIKK的20-1000倍，并且有60种激酶。KU-0060648可提高HDR效率并衰减NHEJ频率。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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NU7026

Catalog No. A12752
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DNA-PK 抑制剂

NU7026是一种新型的在无细胞试验中IC50为0.23 μM，作用于DNA-PK比作用于PI3K选择性高60倍，对ATM和ATR没有抑制活性。可增强用于治疗白血病的拓扑异构酶II毒物的细胞毒性。了解更多

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- Velichko AK, .et al. Hypoosmotic stress induces R loop formation in nucleoli and ATR/ATM-dependent silencing of nucleolar transcription, Nucleic Acids Res, 2019, May 22. pii: gkz436 PMID: 31114877
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CC-115

Catalog No. A15779
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mTOR/DNA-PK 抑制剂

CC-115是mTOR/DNA-PK的抑制剂（IC50 = 21/13 nM）。了解更多

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CCT251545

Catalog No. A16216
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Wnt 抑制剂

CCT251545是口服有效的WNT信号抑制剂，IC50值为5 nM。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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Nedisertib

Catalog No. A17055
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DNA-PK 抑制剂

Nedisertib (M-3814,MSC2490484A)是一种可口服的DNA依赖性蛋白激酶（DNA-PK）抑制剂，具有潜在的抗肿瘤和化学/放射增敏活性。了解更多

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AZD-7648

Catalog No. A20049
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DNA-PK inhibitor

AZD-7648 is a potent and selective DNA-PK inhibitor. Anti-tumor activity. 了解更多

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(Rac)-Nedisertib

Catalog No. A21383
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DNA-PK inhibitor

(Rac)-Nedisertib ((Rac)-M3814) is a racemate of Nedisertib, a potent DNA-PK inhibitor, with an IC50 of <3 nM. 了解更多

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