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NU7026
別名：LY293646
NU7026 (LY293646) is a potent DNA-PK inhibitor with IC50 of 0.23 μM in cell-free assays, 60-fold selective for DNA-PK than PI3K and inactive against both ATM and ATR. NU7026 enhances G2/M cell arrest and apoptosis.
CAS No. 154447-35-5
文献中Selleckの製品使用例（62）
製品安全説明書
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NU7026関連製品
シグナル伝達経路
DNA-PK阻害剤の選択性比較
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | 活性情報 | PMID |
|---|---|---|---|---|---|
| HeLa cells | Function assay | Inhibition of mTOR protein isolated from HeLa cells, IC50=6.4 μM | 15658870 | ||
| HeLa cells | Function assay | Inhibition of DNA dependent protein kinase isolated from HeLa cells, IC50=0.23 μM | 15658870 | ||
| HeLa | Function assay | In vitro inhibition of DNA-dependent protein kinase(DNA-PK) from HeLa (human carcinoma) cells, IC50=0.23μM | 12941339 | ||
| 他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい | |||||
生物活性
| 製品説明 | NU7026 (LY293646) is a potent DNA-PK inhibitor with IC50 of 0.23 μM in cell-free assays, 60-fold selective for DNA-PK than PI3K and inactive against both ATM and ATR. NU7026 enhances G2/M cell arrest and apoptosis. | ||||
|---|---|---|---|---|---|
| Targets |
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| In Vitro | ||||
| In vitro |
NU7026 potentiates ionizing radiation induced cytotoxicity in a concentration-dependent manner in V3YAC and PARP-1+/+ cells. NU7026 completely abolishes potentially lethal damage recovery in growth-arrested cells. NU7026 inhibits DNA DSB repair by 56% in the V3YAC cell line. [1] NU7026 (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. NU7026 (10 μM) also potentiates the growth inhibitory effect in this leukemia cell line with a PF50 value of 10.53. NU7026 (10 μM) enhances the -induced cell cycle G2 blockade in K562 cells. NU7026 potentiates topo II poisons involves inhibition of nonhomologous end joining and a G2/M checkpoint arrest. [2] NU7026 (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. [3] NU7026 (< 10 μM) has synergistic cytotoxic activity at nontoxic doses of NU7026 in a CLL cell line (I83) and in primary CLL-lymphocytes. NU7026 (10 μM) increases -induced G(2)/M arrest in I83 cells. NU7026 (10 μM) enhances -induced γH2AX throughout the cell cycle in the I83 cell line. NU7026 (10 μM) Increases -Induced apoptosis in the I83 cell line. [4] NU7026 (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. [5] |
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|---|---|---|---|---|
| Kinase Assay | Recombinant kinase assay | |||
| 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 NU7026 (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. | ||||
| 細胞実験 | 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 drug for 3 h. |
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| 実験結果図 | Methods | Biomarkers | 結果図 | PMID |
| Western blot | pDNA-PKcs S2056 / DNA-PKcs |
|
22131882 | |
| Growth inhibition assay | Cell viability |
|
26716839 | |
| In Vivo | ||
| 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 NU7026 at dose of 20 mg/kg is 20 and 15%, respectively. [3] |
|
|---|---|---|
| 動物実験 | 動物モデル | Female BALB/c mice |
| 投与量 | 25 mg/kg | |
| 投与経路 | intraperitoneal injection or orally | |
化学情報
| 分子量 | 281.31 | 化学式 | C17H15NO3 |
| CAS No. | 154447-35-5 | SDF | Download NU7026 SDFをダウンロードする |
| Smiles | C1COCCN1C2=CC(=O)C3=C(O2)C4=CC=CC=C4C=C3 | ||
| 保管 | |||
|
In vitro |
4-Methylpyridine : 5 mg/mL DMSO : 1 mg/mL ( (3.55 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。) Water : Insoluble |
モル濃度計算器 |
|
in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | ||||
実験計算
投与溶液組成計算機(クリア溶液)
ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）
mg/kg
g
μL
匹
ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
投与溶媒濃度： mg/ml;
DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )
投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。
投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。
注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。
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