NU7026

製品コードS2893 バッチS289303

印刷

化学情報

Synonyms

LY293646

Storage
(From the date of receipt)

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

化学式

C₁₇H₁₅NO₃

分子量

281.31

CAS No.

154447-35-5

Solubility (25°C)*

体外

DMSO

2 mg/mL (7.1 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	NU7026 (LY293646) は、細胞フリーアッセイにおいてIC50が0.23 µMの強力なDNA-PK阻害剤であり、PI3Kに対しては60倍の選択性を示し、ATMおよびATRの両方に対しては不活性です。NU7026はG2/M細胞周期停止とアポトーシスを促進します。
in vitro	NU7026 potentiates ionizing radiation induced cytotoxicity in a concentration-dependent manner in V3YAC and PARP-1+/+ cells. This compound completely abolishes potentially lethal damage recovery in growth-arrested cells. It inhibits DNA DSB repair by 56% in the V3YAC cell line. This chemical (10 μM) potentiates the growth inhibitory effects of doxorubicin, mAMSA with PF50 values ranging from approximately 19 for mAMSA to approximately 2 in K562 cells. It (10 μM) also potentiates the growth inhibitory effect in this leukemia cell line with a PF50 value of 10.53. This compound (10 μM) enhances the -induced cell cycle G2 blockade in K562 cells. It potentiates topo II poisons involves inhibition of nonhomologous end joining and a G2/M checkpoint arrest. This compound (10 μM) exposure of 4 h in combination with 3 Gy radiation is required for a significant radiosensitisation effect in CH1 human ovarian cancer cells. It (< 10 μM) has synergistic cytotoxic activity at nontoxic doses of this chemical in a CLL cell line (I83) and in primary CLL-lymphocytes. This compound (10 μM) increases -induced G(2)/M arrest in I83 cells. It (10 μM) enhances -induced γH2AX throughout the cell cycle in the I83 cell line. This chemical (10 μM) Increases -Induced apoptosis in the I83 cell line. It (55 μM) results in a dramatic induction of telomere fusion in p53 null MEFs and significantly fewer telomere fusions in p53 and ligase IV double null MEFs.
in vivo	NU7026 (20mg/kg, i.v.) undergoes rapid plasma clearance (0.108/hour) in mice and this is largely attributed to extensive metabolism. Bioavailability following interperitoneal (i.p.) and p.o. administration of this compound at dose of 20 mg/kg is 20 and 15%, respectively.

製品説明

NU7026 (LY293646) は、細胞フリーアッセイにおいてIC50が0.23 µMの強力なDNA-PK阻害剤であり、PI3Kに対しては60倍の選択性を示し、ATMおよびATRの両方に対しては不活性です。NU7026はG2/M細胞周期停止とアポトーシスを促進します。

in vitro

NU7026 potentiates ionizing radiation induced cytotoxicity in a concentration-dependent manner in V3YAC and PARP-1+/+ cells. This compound completely abolishes potentially lethal damage recovery in growth-arrested cells. It inhibits DNA DSB repair by 56% in the V3YAC cell line.

This chemical (10 μM) potentiates the growth inhibitory effects of doxorubicin, mAMSA with PF50 values ranging from approximately 19 for mAMSA to approximately 2 in K562 cells. It (10 μM) also potentiates the growth inhibitory effect in this leukemia cell line with a PF50 value of 10.53. This compound (10 μM) enhances the -induced cell cycle G2 blockade in K562 cells. It potentiates topo II poisons involves inhibition of nonhomologous end joining and a G2/M checkpoint arrest.

This compound (10 μM) exposure of 4 h in combination with 3 Gy radiation is required for a significant radiosensitisation effect in CH1 human ovarian cancer cells.

It (< 10 μM) has synergistic cytotoxic activity at nontoxic doses of this chemical in a CLL cell line (I83) and in primary CLL-lymphocytes. This compound (10 μM) increases -induced G(2)/M arrest in I83 cells. It (10 μM) enhances -induced γH2AX throughout the cell cycle in the I83 cell line. This chemical (10 μM) Increases -Induced apoptosis in the I83 cell line.

It (55 μM) results in a dramatic induction of telomere fusion in p53 null MEFs and significantly fewer telomere fusions in p53 and ligase IV double null MEFs.

in vivo

NU7026 (20mg/kg, i.v.) undergoes rapid plasma clearance (0.108/hour) in mice and this is largely attributed to extensive metabolism. Bioavailability following interperitoneal (i.p.) and p.o. administration of this compound at dose of 20 mg/kg is 20 and 15%, respectively.

プロトコル(参考用のみ)

キナーゼアッセイ	Recombinant kinase assay
キナーゼアッセイ	Mammalian DNA-PK (500 ng/μL) is isolated from HeLa cell nuclear extract after chromatography using Q-Sepharose, S-Sepharose, and Heparin agarose. DNA-PK (250 ng) activity is measured at 30℃, in a final volume of 40 μL, in buffer containing 25 mM HEPES (pH 7.4), 12.5 mM MgCl₂, 50 mM KCl, 1 mM DTT, 10% v/v Glycerol, 0.1% w/v NP-40, and 1 mg of the substrate GST-p53N66 in polypropylene 96-well plates. To the assay mix, varying concentrations of this compound (in DMSO at a final concentration of 1% v/v) are added. After 10 min of incubation, ATP is added to give a final concentration of 50 μM, along with a 30-mer double-stranded DNA oligonucleotide (final concentration of 0.5 ng/mL), to initiate the reaction. After 1 hour with shaking, 150 μL of PBS are added to the reaction, and 5 μL are then transferred to a 96-well opaque white plate containing 45 μl of PBS per well, where the GSTp53N66 substrate is allowed to bind to the wells for 1 hour. The IC50s for the compounds in all of the enzymes assays are derived from sigmoidal plots using the graphic package Prism, in which the enzyme activity in the varying concentration of compounds is plotted against the concentration of compound.
細胞アッセイ	細胞株	A549 cells
	濃度	10 μM
	反応時間	3 h
	実験の流れ	Cells were treated with indicated concentration of this compound for 3 h.
動物実験	動物モデル	Female BALB/c mice
	投薬量	25 mg/kg
	投与方法	intraperitoneal injection or orally

参考

https://pubmed.ncbi.nlm.nih.gov/14522929/
https://pubmed.ncbi.nlm.nih.gov/15010369/
https://pubmed.ncbi.nlm.nih.gov/16249792/

https://pubmed.ncbi.nlm.nih.gov/17351105/
https://pubmed.ncbi.nlm.nih.gov/19244120/
https://pubmed.ncbi.nlm.nih.gov/36280132/

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カスタマーフィードバック

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

: Data from [Data independently produced by , , Clin Cancer Res, 2014, 20(13): 3496-50]

: Data from [Data independently produced by , , Nucleic Acids Res, 2016, 44(21):10259-10276]

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：

Genome rearrangements induced by the stimulation of end-joining of DNA double strand breaks through multiple phosphorylation of MRE11 by the kinase PKB/AKT1 [ Nucleic Acids Res, 2025, 53(11)gkaf468]	PubMed: 40479710
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Noncanonical inhibition of topoisomerase II alpha by oxidative stress metabolites [ Redox Biol, 2025, 80:103504]	PubMed: 39879737
TOX High-Mobility Group Box Family Member 4 promotes DNA double-strand break repair via nonhomologous end joining [ J Biol Chem, 2025, 301(6):110174]	PubMed: 40328361
An open-source pipeline for calcium imaging and all-optical physiology in human stem cell-derived neurons [ bioRxiv, 2025, 2025.07.21.664988]	PubMed: 40777501
Topoisomerase I is an evolutionarily conserved key regulator for satellite DNA transcription [ Nat Commun, 2024, 15(1):5151]	PubMed: 38886382
LC3B drives transcription-associated homologous recombination via direct interaction with R-loops [ Nucleic Acids Res, 2024, gkae156]	PubMed: 38412240
Generation and characterization of six human induced pluripotent stem cell lines (hiPSCs) from three individuals with SSADH Deficiency and CRISPR-corrected isogenic controls [ Stem Cell Res, 2024, 77:103424]	PubMed: 38677032
Topoisomerase I is an Evolutionarily Conserved Key Regulator for Satellite DNA Transcription [ bioRxiv, 2024, 2024.05.03.592391]	PubMed: 38746280
Blocking Genomic Instability Prevents Acquired Resistance to MAPK Inhibitor Therapy in Melanoma [ Cancer Discov, 2023, 13(4):880-909]	PubMed: 36700848

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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