NU7441 (KU-57788) Inhibitor CAS No. 503468-95-9

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Chemical Characteristic

Product Name	NU7441 (KU-57788)
CAS No.	503468-95-9
Molecular Weight	413.49
Formula	C₂₅H₁₉NO₃S
Chemical Name	8-dibenzothiophen-4-yl-2-morpholin-4-ylchromen-4-one
Smiles	c1(cc(=O)c2c(o1)c(ccc2)c1c2c(c3c(s2)cccc3)ccc1)N1CCOCC1
Chemical Structure

Biological activities

NU7441(KU-57788) is a highly potent and selective DNA-PK inhibitor. The IC50 of NU7441(KU-57788) inhibits DNA-PK is 14 nM.^[1] NU7441(KU-57788) also inhibits PI3K with an IC50 of 5 µM.^[2] In vitro, NU7441(KU-57788) inhibits DNA-PK activity after IR stimulation in K562 cells in a concentration-dependent manner.^[3] Meanwhile, NU7441(KU-57788) increases the induction of γH2AX by H2O2 in Rad18-depleted G1 cells.^[4] In vivo, NU7441(KU-57788) shows ATP-competitive inhibition kinetics and increases etoposide-induced tumor growth delay in xenograft models. NU7441(KU-57788) increases levels of fludarabine-induced gH2AX foci and correspondingly decreases fludarabine-induced cell death.^[5] Furthermore, NU7441(KU-57788) enhances the antitumor activity of etoposide in a human colon cancer xenograft model.^[6] NU7441(KU-57788) inhibits UV-induced RPA p34 hyperphosphorylation in a dose-dependent manner both in cells lacking and cells expressing pol.^[7]

Protocols

In vitro, NU7441(KU-57788) is dissolved in DMSO.^[8]

References

[1] Leahy JJ, et al. Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries. Bioorg Med Chem Lett. 2004, 14(24):6083-6087. [2] Zhou T, et al. Tyrosyl-DNA phosphodiesterase and the repair of 3'-phosphoglycolate-terminated DNA double-strand breaks. DNA Repair (Amst). 2009, 8(8):901-911. [3] Tavecchio M, et al. Further characterisation of the cellular activity of the DNA-PK inhibitor, NU7441, reveals potential cross-talk with homologous recombination. Cancer Chemother Pharmacol. 2012, 69(1):155-164. [4] Yang Y, et al. Cell cycle stage-specific roles of Rad18 in tolerance and repair of oxidative DNA damage. Nucleic Acids Res. 2013, 41(4): 2296-2312. [5] Willmore E, et al. DNA-dependent protein kinase is a therapeutic target and an indicator of poor prognosis in B-cell chronic lymphocytic leukemia. Clin Cancer Res. 2008, 14(12):3984-3992. [6] Zhao Y, et al. Preclinical evaluation of a potent novel DNA-dependent protein kinase inhibitor NU7441. Cancer Res. 2006, 66(10):5354-5362. [7] Cruet-Hennequart S, et al. UV-induced RPA phosphorylation is increased in the absence of DNA polymerase eta and requires DNA-PK. DNA Repair (Amst). 2006, 5(4):491-504. [8] Adams BR, et al. Dynamic dependence on ATR and ATM for double-strand break repair in human embryonic stem cells and neural descendants. PLoS One. 2010, 5(4): e10001.

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