NU7026

For research use only.

Catalog No.S2893 Synonyms: LY293646

35 publications

NU7026 Chemical Structure

CAS No. 154447-35-5

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.

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Selleck's NU7026 has been cited by 35 publications

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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

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 idarubicin, daunorubicin, doxorubicin, etoposide, mAMSA, and mitoxantrone with PF50 values ranging from approximately 19 for mAMSA to approximately 2 for idarubicin in K562 cells. NU7026 (10 μM) also potentiates the growth inhibitory effect of etoposide in this leukemia cell line with a PF50 value of 10.53. NU7026 (10 μM) enhances the etoposide-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) plus chlorambucil has synergistic cytotoxic activity at nontoxic doses of NU7026 in a CLL cell line (I83) and in primary CLL-lymphocytes. NU7026 (10 μM) increases chlorambucil-induced G(2)/M arrest in I83 cells. NU7026 (10 μM) enhances chlorambucil -induced γH2AX throughout the cell cycle in the I83 cell line. NU7026 (10 μM) Increases chlorambucil-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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HeLa cells M{\uXGZ2dmO2aX;uJIF{e2G7 Mlz3TY5pcWKrdHnvckBw\iCGTlGg[IVx\W6mZX70JJBzd3SnaX6gb4lv[XOnIHnzc4xifGWmIH\yc40hUGWOYTDj[YxteyxiSVO1NF0xNjJ|IN88US=> NV\ubVhwOTV4NUi4O|A>
HeLa cells MXjGeY5kfGmxbjDhd5NigQ>? M3vyU2lvcGmkaYTpc44hd2ZibWTPVkBxem:2ZXnuJIl{d2yjdHXkJIZzd21iSHXMZUBk\WyuczygTWM2OD14LkSg{txO NGDGe2YyPTZ3OEi3NC=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pDNA-PKcs S2056 / DNA-PKcs ; 

PubMed: 22131882     


Inhibition of DNA-PKcs phosphorylation at serine 2056 was observed from 1 to 50 µM DNA-PK inhibitor NU7026, consistent with DNA-PKcs autophosphorylation at this residue.

22131882
Growth inhibition assay
Cell viability; 

PubMed: 26716839     


Cell viability of NGP cells after co-treatment with NU7026 and IR. Cells were treated with 0, 2, 10 or 20 μM NU7026, 1 h prior to exposure to up to 6.25 Gy IR. At 48, 72, 96 and 120 h after IR-exposure, MTT cell proliferation assays were performed to study inhibitory effects on cell viability. Data represent the mean (n = 4) +/- SD.

26716839
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]

Protocol

Animal Research:[3]
- Collapse
  • Animal Models: Female BALB/c mice
  • Dosages: 25 mg/kg
  • Administration: intraperitoneal injection or orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 1 mg/mL (3.55 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing.
30 mg/mL

* 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.

Chemical Information

Molecular Weight 281.31
Formula

C17H15NO3

CAS No. 154447-35-5
Storage powder
in solvent
Synonyms LY293646
Smiles C1COCCN1C2=CC(=O)C3=C(O2)C4=CC=CC=C4C=C3

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID