Name: NU7441 (KU-57788)
Price: 252.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    NU7441 is a selective inhibitor of DNA-dependent protein kinase (DNA-PK) with IC50 value of 13 nM [1].
    NU7441 is an ATP-competitive inhibitor of DNA-PK and showed a Ki value of 0.65 nM. The inhibition of DNA-PK was selective. NU7441 showed no inhibition effect on the DNA-PK-related enzymes ATM and ATR at concentration of 100 μM. For mTOR and PI3K, NU7441 exerted inhibition activities with IC50 values of 1.7 and 5 μM, respectively, which were about 100-fold higher than the IC50 value of DNA-PK. In HeLa cells, treatment of NU7441 at concentration of 100 nM significantly enhanced the sensitivity of cells to etoposide and promoted cells to death. In mice bearing SW620 xenografts, coadministration of NU7441 and etoposide caused a tumor growth delay of 5.4 days which was twice longer than that caused by etoposide alone [1, 2].
    
    [1] Hardcastle I R, Cockcroft X, Curtin N J, et al. Discovery of potent chromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK) using a small-molecule library approach. Journal of medicinal chemistry, 2005, 48 (24): 7829-7846.
    [2] Zhao Y, Thomas H D, Batey M A, et al. Preclinical evaluation of a potent novel DNA-dependent protein kinase inhibitor NU7441. Cancer research, 2006, 66 (10): 5354-5362.
- Properties
  - Alternative Name
    
    KU 57788; NU-7441; KU57788; NU7441; NU 7441; 8-dibenzothiophen-4-yl-2-morpholin-4-ylchromen-4-one
    
    CAS Number
    
    503468-95-9
    
    Molecular Formula
    
    C25H19NO3S
    
    Molecular Weight
    
    413.49
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in EtOH; insoluble in H2O; ≥4.13 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Kostaras E, Kaserer T, et al. "A systematic molecular and pharmacologic evaluation of AKT inhibitors reveals new insight into their biological activity." Br J Cancer. 2020;10.1038/s41416-020-0889-4. PMID:32439931
    2. Jennifer Risso-Ballester, Rafael Sanjuán. "High Fidelity Deep Sequencing Reveals No Effect of ATM, ATR, and DNA-PK Cellular DNA Damage Response Pathways on Adenovirus Mutation Rate." Viruses 2019, 11(10), 938.
    3. Piekna-Przybylska D, Nagumotu K, et al. "HIV-1 infection renders brain vascular pericytes susceptible to the extracellular glutamate." J Neurovirol. 2018 Nov 6. PMID:30402824
    4. Piekna-Przybylska D, Maggirwar SB. "CD4+ memory T cells infected with latent HIV-1 are susceptible to drugs targeting telomeres." Cell Cycle.2018;17(17):2187-2203. PMID:30198385
    5. Piekna-Przybylska D, Sharma G, et al. "Deficiency in DNA damage response, a new characteristic of cells infected with latent HIV-1." Cell Cycle. 2017 May 19;16(10):968-978. PMID:28388353
    6. Rulina AV, Mittler F, et al. "Distinct outcomes of CRL-Nedd8 pathway inhibition reveal cancer cell plasticity." Cell Death Dis. 2016 Dec 1;7(12):e2505. PMID:27906189

NU7441 (KU-57788)

NU7441 (KU-57788)

Background

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