NU7441 (KU-57788)

NU7441 is a highly potent and selective DNA-PK inhibitor with IC50 of 14 nM and also inhibits PI3K with IC50 of 5 μM.

Price Stock Quantity  
In DMSO USD 112 In stock
USD 70 In stock
USD 120 In stock
USD 370 In stock
USD 970 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

NU7441 (KU-57788) Chemical Structure

NU7441 (KU-57788) Chemical Structure
Molecular Weight: 413.49

Validation & Quality Control

Customer Reviews(2)

Quality Control & MSDS

Related Compound Libraries

NU7441 (KU-57788) is available in the following compound libraries:

DNA-PK inhibitors with Unique Features

  • Non-specific DNA-PK Inhibitor

    PI-103 DNA-PK, IC50=23 nM; p110α/β/δ/γ, IC50=2 nM/3 nM/3 nM/15 nM; mTOR, IC50=30 nM.

  • Most Potent DNA-PK Inhibitor

    PIK-75 DNA-PK, IC50=2 nM.

  • Newest DNA-PK Inhibitor

    KU-0060648 Dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 of 8.6 nM and 4 nM, 0.5 nM, 0.1 nM respectively, less inhibition of PI3Kγ with IC50 of 0.59 μM.

  • Classic DNA-PK Inhibitor

    NU7026 Potent DNA-PK inhibitor with IC50 of 0.23 μM, 60-fold selective for DNA-PK than PI3K and inactive against both ATM and ATR.

Product Information

  • Inhibition Profile
  • Compare DNA-PK Inhibitors
    Compare DNA-PK Inhibitors
  • Research Area
  • Combination Therapy
    Combination Therapy

Product Description

Biological Activity

Description NU7441 is a highly potent and selective DNA-PK inhibitor with IC50 of 14 nM and also inhibits PI3K with IC50 of 5 μM.
Targets DNA-PK
IC50 14 nM [1]
In vitro NU7441 increases the persistence of γH2AX foci after ionizing radiation–induced or etoposide-induced DNA damage. NU7441 (0.5 μM or 1 μM) appreciably increases G2-M accumulation induced by ionizing radiation, etoposide, and doxorubicin in both SW620 and LoVo cells. [2] NU7441 causes persistence of doxorubicin- and ionising radiation-induced DNA double-strand break and also slightly decreases homologous recombination activity DNA-PK-proficient M059-Fus-1 and DNA-PK-deficient M059 J human tumour cells. [3] NU7441 inhibits UV-induced RPA p34 hyperphosphorylation in a dose-dependent manner both in cells lacking and cells expressing polymerase η. [4] NU7441 increases levels of fludarabine-induced γH2AX foci and correspondingly decreased fludarabine-induced cell death in chronic lymphocytic leukemia cells. [5] NU7441 also inhibits mitoxantrone-induced DNA-PKcs autophosphorylation and repair in chronic lymphocytic leukemia cells. [6]
In vivo NU7441 intraperitoneally administrated at dose of 10 mg/kg maintains for at least 4 hours shows nontoxic and increases etoposide-induced tumor growth delay 2-fold in mice bearing SW620 xenografts. [2]
Features

Protocol(Only for Reference)

Cell Assay: [2]

Cell lines SW620, LoVo, V3-YAC and V3 cells
Concentrations 0.5 μM or 1 μM
Incubation Time 17 hours
Method The effect of NU7441 on cellular survival following exposure to etoposide, doxorubicin, and ionizing radiation is measured in SW620, LoVo, V3, and V3-YAC cells by clonogenic assays. Briefly, growing cells in six-well plates or 6-cm dishes are exposed to etoposide or doxorubicin with or without NU7441 (0.5 or 1.0 μM) for 16 hours. For radiosensitization studies, NU7441 is added to the cells 1 hour before irradiation. V3 and V3-YAC cells are exposed to γ-irradiation (3.1 Gy/min 137Cesium). SW620 and LoVo are exposed to X-irradiation (2.9 Gy/min at 230 kV, 10 mA) due to the equipment available. After irradiation, the cells are incubated with or without NU7441 for a further 16 hours. Cells are then harvested by trypsinization, counted, and seeded into 10-cm diameter Petri dishes at densities varying from 100 to 105 per dish in drug-free medium for colony formation. Colonies are stained with crystal violet after 10 to 14 days and counted with an automated colony counter. The survival reduction factor (SRF) is calculated as the surviving fraction of cells in the absence of NU7441 divided by the surviving fraction of cells in the presence of NU7441 for any given dose or concentration of cytotoxic agent. The dose modification ratio (DMR90) is calculated as the concentration/dose of cytotoxic agent required to kill 90% of the cells in the absence of NU7441 divided by the concentration/dose of cytotoxic agent required to kill 90% of the cells in the presence of NU7441.

Animal Study: [2]

Animal Models Female rude mice bearing SW620 xenografts
Dosages 10 mg/kg
Administration Intraperitoneally administrated
1

References

Chemical Information

Download NU7441 (KU-57788) SDF
Molecular Weight (MW) 413.49
Formula

C25H19NO3S

CAS No. 503468-95-9
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Syonnyms N/A
Solubility (25°C) * In vitro DMSO 3 mg/mL (7 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name 4H-1-Benzopyran-4-one, 8-(4-dibenzothienyl)-2-(4-morpholinyl)-

Research Area

Customer Reviews (2)


Click to enlarge
Rating
Source Nucleic Acids Research, 2013, 1–13. NU7441 (KU-57788) purchased from Selleck
Method Confocal immunostaining
Cell Lines 293T
Concentrations
Incubation Time 30min ,60min
Results the number of IRIFs was reduced significantly in p18CycE-expressing HEK 293T cells compared with parental cells. Pharmacological inhibition of ATM with KU55933 Revealed that S25-53BP1 phosphorylation was ATM-dependent in these cells as IRIFs of S25-53BP1 were abolished in both parental, as well as p18CycE-expressing cells.

Click to enlarge
Rating
Source Dr. Zhang of Tianjin Medical University. NU7441 (KU-57788) purchased from Selleck
Method
Cell Lines A549 cells
Concentrations 0-10 μM
Incubation Time 3 h
Results NU-7441 treatment resulted in a reduction of AKT phosphorylation.

Product Citations (4)

Tech Support & FAQs

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.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related DNA-PK Inhibitors

  • KU-0060648

    KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 of 8.6 nM and 4 nM, 0.5 nM, 0.1 nM respectively, less inhibition of PI3Kγ with IC50 of 0.59 μM.

  • VE-821

    VE-821 is a potent and selective ATP competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM, shows inhibition of H2AX phosphorylation, minimal activity against PIKKs ATM, DNA-PK, mTOR and PI3Kγ.

  • AZD5363

    AZD5363 potently inhibits all isoforms of Akt(Akt1/Akt2/Akt3) with IC50 of 3 nM/8 nM/8 nM, similar to P70S6K/PKA and lower activity towards ROCK1/2. Phase 1/2.

    Features:Moderate preclinical tolerability, and PD characteristics of an AKT inhibitor. Distinct profile from other AKT inhibitors in clinical development.

  • NU7441 (KU-57788)

    NU7441 is a highly potent and selective DNA-PK inhibitor with IC50 of 14 nM and also inhibits PI3K with IC50 of 5 μM.

  • NU7026

    NU7026 is a potent DNA-PK inhibitor with IC50 of 0.23 μM, 60-fold selective for DNA-PK than PI3K and inactive against both ATM and ATR.

  • MK-2206 2HCl

    MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, respectively; no inhibitory activities against 250 other protein kinases observed. Phase 2.

    Features:The first allosteric small molecule inhibitor of Akt to enter clinical development.

  • BEZ235 (NVP-BEZ235, Dactolisib)

    BEZ235 (NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM/5 nM/7 nM/75 nM/6 nM, respectively. Inhibits ATR with IC50 of 21 nM; shown to be poor inhibitory to Akt and PDK1. Phase 1/2.

  • Rapamycin (Sirolimus)

    Rapamycin (Sirolimus, AY-22989, WY-090217) is a specific mTOR inhibitor with IC50 of ~0.1 nM.

  • Everolimus (RAD001)

    Everolimus (RAD001) is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM.

  • GDC-0941

    GDC-0941 is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).

Recently Viewed Items

Tags: buy NU7441 (KU-57788) | NU7441 (KU-57788) supplier | purchase NU7441 (KU-57788) | NU7441 (KU-57788) cost | NU7441 (KU-57788) manufacturer | order NU7441 (KU-57788) | NU7441 (KU-57788) distributor
Contact Us