1. Cell Cycle/DNA Damage
    PI3K/Akt/mTOR
  2. DNA-PK
  3. NU 7026

NU 7026 (Synonyms: LY293646)

Cat. No.: HY-15719 Purity: 99.95%
Handling Instructions

NU 7026 (LY293646) is a novel specific DNA-PK inhibitor with IC50 of 0.23 μM, also inhibits PI3K with IC50 of 13 μM.

For research use only. We do not sell to patients.

NU 7026 Chemical Structure

NU 7026 Chemical Structure

CAS No. : 154447-35-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 96 In-stock
Estimated Time of Arrival: December 31
50 mg USD 384 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 6 publication(s) in Google Scholar

Top Publications Citing Use of Products

    NU 7026 purchased from MCE. Usage Cited in: Cell Mol Life Sci. 2019 Feb 6.

    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 MCE. Usage Cited in: Cell Mol Life Sci. 2019 Feb 6.

    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.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    NU 7026 (LY293646) is a novel specific DNA-PK inhibitor with IC50 of 0.23 μM, also inhibits PI3K with IC50 of 13 μM.

    IC50 & Target[1]

    DNA-PK

    0.23 μM (IC50)

    PI3K

    13 μM (IC50)

    In Vitro

    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].

    In Vivo

    NU7026, a novel inhibitor of the DNA repair enzyme DNA-dependent protein kinase (DNA-PK). Following intravenous administration to mice at 5 mg/kg, NU7026 underwent rapid plasma clearance (0.108 L/h) and this is largely attributed to extensive metabolism. Bioavailability following interperitoneal (i.p.) and p.o. administration at 20 mg/kg is 20 and 15%, respectively[3].
    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].

    Molecular Weight

    281.31

    Formula

    C₁₇H₁₅NO₃

    CAS No.

    154447-35-5

    SMILES

    O=C1C2=CC=C3C=CC=CC3=C2OC(N4CCOCC4)=C1

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 2.9 mg/mL (10.31 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.5548 mL 17.7740 mL 35.5480 mL
    5 mM 0.7110 mL 3.5548 mL 7.1096 mL
    10 mM 0.3555 mL 1.7774 mL 3.5548 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Kinase Assay
    [1]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [2]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3]

    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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
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    NU 7026
    Cat. No.:
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