NU5455 | DNA-PK inhibitor | Probechem Biochemicals

Chemical Structure : NU5455

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NU5455 (NU 5455, NU-5455)

货号: PC-72041Not For Human Use, Lab Use Only.

NU5455 (NU-5455) is a potent, highly selective, oral inhibitor of DNA-dependent protein kinase catalytic subunit (DNA-PKcs) activity with IC50 of 8.2 nM.

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生物&药学活性

NU5455 (NU-5455) is a potent, highly selective, oral inhibitor of DNA-dependent protein kinase catalytic subunit (DNA-PKcs) activity with IC50 of 8.2 nM.
NU5455 displays selectivity versus Vps34 (8.7-fold), PI3Kδ (33.7-fold), ATM/ATR (both >1200-fold), 228-fold selectivity margin for DNA-PKcs kinase activity versus that of PI3Kα.
NU5455 inhibited radiation-induced activation of DNA-PK with an IC50 of 168 nM, but did not inhibit IGF-stimulated activation of AKT in MCF7 cells even at 10 uM.
NU5455 inhibited the repair of DNA-DSBs induced by treatment with enzyme AfeI or ScaI restriction endonucleases within a 24-hour period in HEK293T cells, significantly increased the number of colocalized γH2AX and 53BP1 foci.
NU5455 is a highly selective inhibitor of DNA-PKcs that is active in cells and that can perturb DNA-DSB repair by NHEJ.
NU5455 preferentially augmented radiotherapy in subcutaneous Calu-6 and A549 lung tumor xenografts, increased both the efficacy and the toxicity of a parenterally administered topoisomerase inhibitor, NU5455 enhanced the activity of doxorubicin released locally in liver tumor xenografts without inducing any adverse effect.

物理化学性质&存储条件

分子量	595.714
分子式	C34H33N3O5S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(6-(2-(8-oxa-3-azabicyclo[3.2.1]octan-3-yl)-4-oxo-4H-chromen-8-yl)dibenzo[b,d]thiophen-2-yl)-N-methyl-2-morpholinoacetamide

参考文献

1. Willoughby CE, et al. J Clin Invest. 2020 Jan 2;130(1):258-271.

2. Jiang Y, et al. Mol Cancer Ther. 2021 Sep;20(9):1663-1671.

NU5455 (NU 5455, NU-5455)

生物&药学活性

物理化学性质&存储条件

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NU5455 (NU 5455, NU-5455)

生物&药学活性

物理化学性质&存储条件

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