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Formula | C25H19NO3S |
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Molecular Weight | 413.49 | CAS No. | 503468-95-9 | ||||
Solubility (25°C)* | In vitro | DMSO | 5 mg/mL (12.09 mM) | ||||
Water | Insoluble | ||||||
Ethanol | Insoluble | ||||||
In vivo (Add solvents to the product individually and in order) |
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* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | NU7441 (KU-57788) is a highly potent and selective DNA-PK inhibitor with IC50 of 14 nM and also inhibits mTOR and PI3K with IC50 of 1.7 μM and 5 μM in cell-free assays, respectively. It reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage. | ||||||
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In vitro | NU7441 increases the persistence of γH2AX foci after ionizing radiation–induced DNA damage. NU7441 (0.5 μM or 1 μM) appreciably increases G2-M accumulation induced by ionizing radiation, 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 -induced γH2AX foci and correspondingly decreased -induced cell death in chronic lymphocytic leukemia cells. [5] NU7441 also inhibits -induced DNA-PKcs autophosphorylation and repair in chronic lymphocytic leukemia cells. [6] It reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage[7]. |
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In vivo | NU7441 intraperitoneally administrated at dose of 10 mg/kg maintains for at least 4 hours shows nontoxic and increases induced tumor growth delay 2-fold in mice bearing SW620 xenografts. [2] |
Cell Assay: |
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Animal Study: |
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Data from [Data independently produced by Toxicol Sci, 2014, 10.1093/toxsci/kfu207]
Data from [Data independently produced by Nucleic Acids Res, 2013, 41(15), 7378-86]
Data from [Nucleic Acids Res, 2013, 41, 10157-69]
, , Dr. Zhang of Tianjin Medical University
Transcription-coupled DNA-protein crosslink repair by CSB and CRL4CSA-mediated degradation [ Nat Cell Biol, 2024, 10.1038/s41556-024-01394-y] | PubMed: 38600236 |
Distinct regulation of ATM signaling by DNA single-strand breaks and APE1 [ Nat Commun, 2024, 15(1):6517] | PubMed: 39112456 |
Comprehensive multi-omics analysis reveals WEE1 as a synergistic lethal target with hyperthermia through CDK1 super-activation [ Nat Commun, 2024, 15(1):2089] | PubMed: 38453961 |
Kaposi's sarcoma herpesvirus exploits the DNA damage response to circularize its genome [ Nucleic Acids Res, 2024, gkad1224] | PubMed: 38180827 |
Switch-like phosphorylation of WRN integrates end-resection with RAD51 metabolism at collapsed replication forks [ Nucleic Acids Res, 2024, gkae807] | PubMed: 39315694 |
The DNA-dependent protein kinase catalytic subunit exacerbates endotoxemia-induced myocardial microvascular injury by disrupting the MOTS-c/JNK pathway and inducing profilin-mediated lamellipodia degradation [ Theranostics, 2024, 14(4):1561-1582] | PubMed: 38389837 |
DNA-PKcs Phosphorylates Cofilin2 to Induce Endothelial Dysfunction and Microcirculatory Disorder in Endotoxemic Cardiomyopathy [ Research (Wash D C), 2024, 7:0331] | PubMed: 38550779 |
DNA-PKcs/AKT1 inhibits epithelial-mesenchymal transition during radiation-induced pulmonary fibrosis by inducing ubiquitination and degradation of Twist1 [ Clin Transl Med, 2024, 14(5):e1690] | PubMed: 38760896 |
DNA damage remodels the MITF interactome to increase melanoma genomic instability [ Genes Dev, 2024, 38(1-2):70-94] | PubMed: 38316520 |
SMARCAL1 ubiquitylation controls its association with RPA-coated ssDNA and promotes replication fork stability [ PLoS Biol, 2024, 22(3):e3002552] | PubMed: 38502677 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.