NU 7026
Based on 14 publication(s) in Google Scholar
NU 7026 (LY293646) is a novel specific DNA-PK inhibitor with IC50 of 0.23 μM, also inhibits PI3K with IC50 of 13 μM.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.97%
- CAS. Nr.: 154447-35-5
- Formel: C17H15NO3
- Molecular Weight:281.31
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Apoptosis Compound Library
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Publications Citing Use of MedChemExpress (MCE) NU 7026
More- Mol Cell. 2022 Jun 2;82(11):2032-2049.e7. [Abstract]
- Nat Commun. 2020 Dec 3;11(1):6182. [Abstract]
- Nucleic Acids Res. 2023 Feb 22;51(3):1154-1172. [Abstract]
- Cell Death Dis. 2022 Apr 25;13(4):404. [Abstract]
- Cell Syst. 2020 Jan 22;10(1):66-81.e11. [Abstract]
- PLoS Biol. 2026 Feb 2;24(2):e3003621. [Abstract]
- Cell Mol Life Sci. 2019 May;76(10):2015-2030. [Abstract]
- Genome Res. 2021 Mar;31(3):461-471. [Abstract]
- Int J Mol Sci. 2022 Jul 7;23(14):7518. [Abstract]
- Sci Rep. 2019 Oct 3;9(1):14257. [Abstract]
- State University of New York at Stony Brook. 2026.
- Res Sq. 2026 Jan 11.
- bioRxiv. 2025 Jun 17:2025.06.16.659978. [Abstract]
- Technische Universitat Darmstadt. 2022 Aug.
Customer Validation & Images
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ELISA
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RT-PCR
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RT-PCR
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Biologische Aktivität
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DNA-PK 0.23 μM (IC50) |
PI3K 13 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
0.23 μM
Compound: 2
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In vitro inhibition of DNA-dependent protein kinase(DNA-PK) from HeLa (human carcinoma) cells.
In vitro inhibition of DNA-dependent protein kinase(DNA-PK) from HeLa (human carcinoma) cells.
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[PMID: 12941339] |
| HeLa | IC50 |
0.23 μM
Compound: 3
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Inhibition of DNA dependent protein kinase isolated from HeLa cells
Inhibition of DNA dependent protein kinase isolated from HeLa cells
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[PMID: 15658870] |
| HeLa | IC50 |
230 nM
Compound: 4
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Inhibition of DNA-PK isolated from human HeLa cell extract assessed as reduction in p53 Ser15 phosphorylation by chemiluminescence assay
Inhibition of DNA-PK isolated from human HeLa cell extract assessed as reduction in p53 Ser15 phosphorylation by chemiluminescence assay
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[PMID: 21080722] |
| HeLa | IC50 |
6.4 μM
Compound: 3
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Inhibition of mTOR protein isolated from HeLa cells
Inhibition of mTOR protein isolated from HeLa cells
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[PMID: 15658870] |
NU7026 (10 μM) potentiates ionizing radiation (IR) cytotoxicity [potentiation factor at 90% cell kill (PF90)=1.51±0.04] in exponentially growing DNA-PK proficient but not deficient cells[1]. NU7026 synergistically sensitizes I83 cells to Chlorambucil (CLB) 3.5-fold[2].NU7026, a novel inhibitor of the DNA repair enzyme DNA-dependent protein kinase (DNA-PK). At a dose of 10 μM, which is nontoxic to cells per se, a minimum NU7026 exposure of 4 h in combination with 3 Gy radiation is required for a significant radiosensitisation effect in CH1 human ovarian cancer cells[3].
Solution in vitro: NU7026 is dissolved in anhydrous DMSO. NU7026 is added to cells to a final concentration of 0.25% DMSO (v/v)[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Solution in vivo:
NU7026 is formulated in 10% DMSO and 5% Tween 20 in saline (i.p. and p.o.) (Mice)[3].
NU7026 is formulated in 10% ethanol, 25% PEG 200 and 5% Tween 20 in saline (i.v.)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 154447-35-5
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Appearance Solid
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Molecular Weight 281.31
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Formel C17H15NO3
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Color Off-white to light yellow
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SMILES
O=C1C2=CC=C3C=CC=CC3=C2OC(N4CCOCC4)=C1
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Synonyms
LY293646
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (14)
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Journal Impact Factor
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Most Recent
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Mol Cell
Cytoplasmic PARP1 links the genome instability to the inhibition of antiviral immunity through PARylating cGAS. [Abstract]2022 Jun 2;82(11):2032-2049.e7. PMID: 35460603 -
Nat Commun
2020 Dec 3;11(1):6182. PMID: 33273464
NU 7026 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Dec 3;11(1):6182. [Abstract]
THP-1 were treated with Nu7026 (10 μM) and infected with HSV-1 or VSV (MOI = 5). Infected cells were harvested at 6 hpi, and the expression of the indicated cytokine genes was analyzed by real-time PCR. NU7026 efficiently increased the expression of innate immune genes induced by HSV-1 and VSV.
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Nucleic Acids Res
Phosphorylation of TRF2 promotes its interaction with TIN2 and regulates DNA damage response at telomeres. [Abstract]2023 Feb 22;51(3):1154-1172. PMID: 36651296 -
Cell Death Dis
PRKDC promotes hepatitis B virus transcription through enhancing the binding of RNA Pol II to cccDNA. [Abstract]2022 Apr 25;13(4):404. PMID: 35468873
NU 7026 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Apr 25;13(4):404. [Abstract]
HBeAg and HBsAg concentrations in the culture supernatants of HBV-infected HepG2-NTCP cells treated with a concentration gradient of NU 7026 (5-20 μM; 24 h pretreatment, HBV infection for 24 h) were detected by ELISA. NU7026 significantly reduced HBeAg and HBsAg secretion.
NU 7026 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Apr 25;13(4):404. [Abstract]
NU 7026 (5-20 μM; 24 h pretreatment, HBV infection for 24 h). Total HBV RNA and pgRNA transcriptions were analyzed by real-time PCR using specific primers. The accumulation of HBV RNAs and pgRNA was inhibited significantly.
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Cell Syst
Torin2 Exploits Replication and Checkpoint Vulnerabilities to Cause Death of PI3K-Activated Triple-Negative Breast Cancer Cells. [Abstract]2020 Jan 22;10(1):66-81.e11. PMID: 31812693 -
PLoS Biol
DNA damage induced by HIV-1 Vpr triggers epigenetic remodeling and transcriptional programs to enhance virus transcription and latency reactivation. [Abstract]2026 Feb 2;24(2):e3003621. PMID: 41628238 -
Cell Mol Life Sci
IGFBP-3 interacts with NONO and SFPQ in PARP-dependent DNA damage repair in triple-negative breast cancer. [Abstract]2019 May;76(10):2015-2030. PMID: 30725116
NU 7026 purchased from MedChemExpress. Usage Cited in: Cell Mol Life Sci. 2019 May;76(10):2015-2030. [Abstract]
Western blots of NONO and SFPQ in MDA-MB-468 cell lysates immunoprecipitated with IGFBP-3-Fab beads, showing that incubation overnight with 20 μM NU7026 block the formation of IGFBP-3 complexes with NONO and SFPQ formed in response to 20 μM etopside.
NU 7026 purchased from MedChemExpress. Usage Cited in: Cell Mol Life Sci. 2019 May;76(10):2015-2030. [Abstract]
Western blots of NONO and SFPQ in MDA-MB-468 cell lysates immunoprecipitated with IGFBP-3-Fab beads, showing that incubation overnight with 20 μM NU7026 block the formation of IGFBP-3 complexes with NONO and SFPQ formed in response to 20 μM etopside.
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Genome Res
2021 Mar;31(3):461-471. PMID: 33574136 -
Int J Mol Sci
Chloroquine-Induced DNA Damage Synergizes with Nonhomologous End Joining Inhibition to Cause Ovarian Cancer Cell Cytotoxicity. [Abstract]2022 Jul 7;23(14):7518. PMID: 35886866 -
Sci Rep
HERC2 regulates RPA2 by mediating ATR-induced Ser33 phosphorylation and ubiquitin-dependent degradation. [Abstract]2019 Oct 3;9(1):14257. PMID: 31582797 -
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bioRxiv
2025 Jun 17:2025.06.16.659978. PMID: 40667017 -
Lösungsmittel & Löslichkeit
DMSO : 2.5 mg/mL (8.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Protokoll
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°C, 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 (the NH2-terminal 66 amino acid residues of human wild-type p53 fused to glutathione S-transferase) in polypropylene 96-well plates. To the assay mix, varying concentrations of inhibitor (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 h 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 h. To detect the phosphorylation event on the serine 15 residue of p53 elicited by DNA-PK, a p53 phosphoserine-15 antibody is used in a basic ELISA procedure. An antirabbit horseradish peroxidase-conjugated secondary antibody is then used in the ELISA before the addition of chemiluminescence reagent to detect the signal as measured by chemiluminescent counting via a TopCount NXT[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
I83 cells are plated in RPMI 1640 medium with 10% FBS (1.5×105 cells/mL) and treated with vehicle (DMSO), 5 μM CLB, CLB IC50, 10 μM NU7026, or the combination of both drugs for 0, 6, 24, and 48 h. Cell cycle distribution, apoptosis, DNA-PK phosphorylation, and γH2AX determination are determined, and they are expressed as a percentage of cells in each phase of the cycle. DNA content is analyzed with a FACSCalibur flow cytometer equipped with CellQuest software[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[3]
Female BALB/c mice are used. NU7026 is formulated in 10% DMSO and 5% Tween 20 in saline for i.p. and perorally (p.o.) administration at 20 and 50 mg/kg, respectively. For i.v. dosing at 5 mg/kg, NU7026 is formulated in 10% ethanol, 25% PEG 200 and 5% Tween 20 in saline. Control animals receive the vehicle alone. Groups of three mice are injected per time point. Blood is collected by cardiac puncture following transient anaesthesia with halothane at 0.083, 0.25, 0.5, 1, 2, 4, 6, and 24 h post administration. Following centrifugation at 1500 g for 2 min to obtain plasma, samples are stored at −20°C until analysis. For urinary excretion studies, NU7026 is administered at 5 mg/kg i.v. Urine is collected over 24 h in metabolic cages, and stored at −20°C until required.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (285 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Veuger SJ, et al. Radiosensitization and DNA repair inhibition by the combined use of novel inhibitors of DNA-dependent protein kinase and poly(ADP-ribose) polymerase-1. Cancer Res. 2003 Sep 15;63(18):6008-15. [Content Brief]
[2]. Amrein L, et al. Chlorambucil cytotoxicity in malignant B lymphocytes is synergistically increased by 2-(morpholin-4-yl)-benzo[h]chomen-4-one (NU7026)-mediated inhibition of DNA double-strand break repair via inhibition of DNA-dependent protein kinase. J [Content Brief]
[3]. Nutley BP, et al. Preclinical pharmacokinetics and metabolism of a novel prototype DNA-PK inhibitor NU7026. Br J Cancer. 2005 Oct 31;93(9):1011-8. [Content Brief]
[4]. Ciszewski WM, et al. Interleukin-4 enhances PARP-dependent DNA repair activity in vitro. J Interferon Cytokine Res. 2014 Sep;34(9):734-40. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.5548 mL | 17.7740 mL | 35.5480 mL | 88.8699 mL |
| 5 mM | 0.7110 mL | 3.5548 mL | 7.1096 mL | 17.7740 mL |
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