Home DNA Damage/DNA Repair DNA-PK inhibitor - PI3K inhibitor - Apoptosis related activator NU7026 For research use only.

NU7026

Synonyms: 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.

NU7026 Chemical Structure

NU7026 Chemical Structure

CAS No. 154447-35-5

Purity & Quality Control

NU7026 Related Products

Signaling Pathway

DNA-PK Signaling Pathways

DNA-PK Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HeLa cells Function assay Inhibition of DNA dependent protein kinase isolated from HeLa cells, IC50=0.23 μM 15658870
HeLa cells Function assay Inhibition of mTOR protein isolated from HeLa cells, IC50=6.4 μM 15658870
HeLa Function assay In vitro inhibition of DNA-dependent protein kinase(DNA-PK) from HeLa (human carcinoma) cells, IC50=0.23μM 12941339
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Biological Activity

Description 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
DNA-PK [1]
(Cell-free assay)		 PI3K [1]
(Cell-free assay)
0.23 μM 13 μM
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]
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.
Cell Research Cell lines A549 cells
Concentrations 10 μM
Incubation Time 3 h
Method

Cells were treated with indicated concentration of drug for 3 h.
Experimental Result Images Methods Biomarkers Images 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]
Animal Research Animal Models Female BALB/c mice
Dosages 25 mg/kg
Administration intraperitoneal injection or orally

Chemical Information & Solubility

Molecular Weight 281.31 Formula

C17H15NO3
CAS No. 154447-35-5 SDF Download NU7026 SDF
Smiles C1COCCN1C2=CC(=O)C3=C(O2)C4=CC=CC=C4C=C3
Storage (From the date of receipt)

In vitro
Batch:

4-Methylpyridine : 5 mg/mL

DMSO : 1 mg/mL ( (3.55 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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