NU7441 (KU-57788)

製品コードS2638 バッチS263804

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₅H₁₉NO₃S

分子量

413.49

CAS No.

503468-95-9

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

3 mg/mL (7.25 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	NU7441 (KU-57788) is a highly potent and selective DNA-PK inhibitor with IC50 of 14 nM and also inhibits mTOR and PI3K with IC50 of 1.7 μM and 5 μM in cell-free assays, respectively. It reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage.
in vitro	NU7441 (KU-57788) increases the persistence of γH2AX foci after ionizing radiation–induced DNA damage. It (0.5 μM or 1 μM) appreciably increases G2-M accumulation induced by ionizing radiation, and doxorubicin in both SW620 and LoVo cells. ^[2] This compound causes persistence of doxorubicin- and ionising radiation-induced DNA double-strand break and also slightly decreases homologous recombination activity DNA-PK-proficient M059-Fus-1 and DNA-PK-deficient M059 J human tumour cells. ^[3] It inhibits UV-induced RPA p34 hyperphosphorylation in a dose-dependent manner both in cells lacking and cells expressing polymerase η. ^[4] NU7441 increases levels of -induced γH2AX foci and correspondingly decreased -induced cell death in chronic lymphocytic leukemia cells. ^[5] It also inhibits -induced DNA-PKcs autophosphorylation and repair in chronic lymphocytic leukemia cells. ^[6] This compound reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage^[7].
in vivo	NU7441 (KU-57788) intraperitoneally administrated at dose of 10 mg/kg maintains for at least 4 hours shows nontoxic and increases induced tumor growth delay 2-fold in mice bearing SW620 xenografts. ^[2]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	SW620, LoVo, V3-YAC and V3 cells
	濃度	0.5 μM or 1 μM
	反応時間	17 hours
	実験の流れ	The effect of NU7441 (KU-57788) on cellular survival following exposure to doxorubicin and ionizing radiation is measured in SW620, LoVo, V3, and V3-YAC cells by clonogenic assays. Briefly, growing cells in six-well plates or 6-cm dishes are exposed to doxorubicin with or without this compound (0.5 or 1.0 μM) for 16 hours. For radiosensitization studies, it is added to the cells 1 hour before irradiation. V3 and V3-YAC cells are exposed to γ-irradiation (3.1 Gy/min ¹³⁷Cesium). SW620 and LoVo are exposed to X-irradiation (2.9 Gy/min at 230 kV, 10 mA) due to the equipment available. After irradiation, the cells are incubated with or without NU7441 for a further 16 hours. Cells are then harvested by trypsinization, counted, and seeded into 10-cm diameter Petri dishes at densities varying from 100 to 10⁵ per dish in drug-free medium for colony formation. Colonies are stained with crystal violet after 10 to 14 days and counted with an automated colony counter. The survival reduction factor (SRF) is calculated as the surviving fraction of cells in the absence of it divided by the surviving fraction of cells in the presence of it for any given dose or concentration of cytotoxic agent. The dose modification ratio (DMR90) is calculated as the concentration/dose of cytotoxic agent required to kill 90% of the cells in the absence of this compound divided by the concentration/dose of cytotoxic agent required to kill 90% of the cells in its presence.
動物実験	動物モデル	Female rude mice bearing SW620 xenografts
	投薬量	10 mg/kg
	投与方法	Intraperitoneally administrated

参考

https://pubmed.ncbi.nlm.nih.gov/15546735/
https://pubmed.ncbi.nlm.nih.gov/16707462/
https://pubmed.ncbi.nlm.nih.gov/21630086/

https://pubmed.ncbi.nlm.nih.gov/16520097/
https://pubmed.ncbi.nlm.nih.gov/18559621/
https://pubmed.ncbi.nlm.nih.gov/21083655/
https://pubmed.ncbi.nlm.nih.gov/26307031/

+ 展开

カスタマーフィードバック

: Data from [Data independently produced by Toxicol Sci, 2014, 10.1093/toxsci/kfu207]

: Data from [Data independently produced by Nucleic Acids Res, 2013, 41(15), 7378-86]

: Data from [Nucleic Acids Res, 2013, 41, 10157-69]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Homologous recombination promotes non-immunogenic mitotic cell death upon DNA damage [ Nat Cell Biol, 2025, 27(1):59-72]	PubMed: 39805921
Highly efficient prime editors for mammalian genome editing based on porcine retrovirus reverse transcriptase [ Trends Biotechnol, 2025, S0167-7799(25)00314-2]	PubMed: 40885667
Phosphorylation-dependent WRN-RPA interaction promotes recovery of stalled forks at secondary DNA structure [ Nat Commun, 2025, 16(1):997]	PubMed: 39870632
Autophosphorylation of the Tousled-like kinases TLK1 and TLK2 regulates recruitment to damaged chromatin via PCNA interaction [ Nucleic Acids Res, 2025, 53(4)gkae1279]	PubMed: 39727191
Homeodomain protein PRRX1 anchors the Ku heterodimers at DNA double-strand breaks to promote nonhomologous end-joining [ Nucleic Acids Res, 2025, 53(6)gkaf200]	PubMed: 40114375
Nuclear damage-induced DNA damage response coupled with IFI16-driven ECM remodeling underlies dilated cardiomyopathy [ Theranostics, 2025, 15(12):5998-6021]	PubMed: 40365289
Cross-species analysis of the nuclease Artemis highlights its evolving function in domesticating RAG-like transposons and residues that are crucial for activity [ PLoS Biol, 2025, 23(4):e3003056]	PubMed: 40245028
DSCC1 restrains 53BP1/RIF1 signaling at DNA double-strand breaks to promote homologous recombination repair [ Cell Rep, 2025, 44(4):115452]	PubMed: 40117291
Defective homologous recombination and genomic instability predict increased responsiveness to carbon ion radiotherapy in pancreatic cancer [ NPJ Precis Oncol, 2025, 9(1):20]	PubMed: 39824957
Extracellular Mitochondria Exacerbate Retinal Pigment Epithelium Degeneration in Diabetic Retinopathy [ Diabetes, 2025, 74(3):409-415]	PubMed: 39715576

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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