NU-7441

• CAT Number: I003781
• CAS Number: 503468-95-9
• Molecular Formula: CHNOS
• Molecular Weight: 413.49
• Purity: ≥95%
• Synonyms: KU-57788; 8-dibenzothiophen-4-yl-2-morpholin-4-ylchromen-4-one
• Target: PI3K/Akt/mTOR
• Solubility: DMSO ≥4.8mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL
• Storage: Store at -20C
• IC50: 14 nM (DNA-PK); 1/3.5 uM(BRD4/BRDT)
• InChI: InChI=1S/C25H19NO3S/c27-21-15-23(26-11-13-28-14-12-26)29-24-17(6-3-9-20(21)24)19-8-4-7-18-16-5-1-2-10-22(16)30-25(18)19/h1-10,15H,11-14H2
• InChIKey: JAMULYFATHSZJM-UHFFFAOYSA-N
• SMILES: C1COCCN1C2=CC(=O)C3=C(O2)C(=CC=C3)C4=CC=CC5=C4SC6=CC=CC=C56

NU-7441(CAT: I003781), also known as KU-57788, is a potent and selective inhibitor of DNA-dependent protein kinase (DNA-PK). DNA-PK is an enzyme involved in the repair of DNA double-strand breaks and plays a critical role in the maintenance of genomic stability. By inhibiting DNA-PK, NU-7441 disrupts the repair pathway, leading to the accumulation of DNA damage and promoting cell death in cancer cells. NU-7441 has been investigated for its potential as a radiosensitizer in cancer therapy, as it enhances the sensitivity of tumor cells to radiation. It has also shown promise in combination with other anticancer agents, including chemotherapy drugs and PARP inhibitors.

Reference

1: Yanai M, Makino H, Ping B, Takeda K, Tanaka N, Sakamoto T, Yamaguchi K, Kodani
M, Yamasaki A, Igishi T, Shimizu E. DNA-PK Inhibition by NU7441 Enhances
Chemosensitivity to Topoisomerase Inhibitor in Non-Small Cell Lung Carcinoma
Cells by Blocking DNA Damage Repair. Yonago Acta Med. 2017 Mar 9;60(1):9-15.
eCollection 2017 Mar. PubMed PMID: 28331416; PubMed Central PMCID: PMC5355839.
2: Sunada S, Kanai H, Lee Y, Yasuda T, Hirakawa H, Liu C, Fujimori A, Uesaka M,
Okayasu R. Nontoxic concentration of DNA-PK inhibitor NU7441 radio-sensitizes
lung tumor cells with little effect on double strand break repair. Cancer Sci.
2016 Sep;107(9):1250-5. doi: 10.1111/cas.12998. Epub 2016 Sep 1. PubMed PMID:
27341700; PubMed Central PMCID: PMC5021029.
3: Yang C, Wang Q, Liu X, Cheng X, Jiang X, Zhang Y, Feng Z, Zhou P. NU7441
Enhances the Radiosensitivity of Liver Cancer Cells. Cell Physiol Biochem.
2016;38(5):1897-905. doi: 10.1159/000445551. Epub 2016 May 9. PubMed PMID:
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Sinkorova Z. Radio-sensitization of human leukaemic MOLT-4 cells by DNA-dependent
protein kinase inhibitor, NU7441. Radiat Environ Biophys. 2014 Mar;53(1):83-92.
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sensitizes breast cancer cells to ionizing radiation and doxorubicin. Breast
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Smith GC. Identification of a highly potent and selective DNA-dependent protein
kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries. Bioorg
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