KU-60019

- Overview
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    Background
    
    KU-60019 is a selective inhibitor of the Ataxia telangiectasia (A-T) mutated (ATM) protein with an IC50 value of 6.3 nM. In literature report, KU-60019 radiosensitizes h-TERT-immortalized normal fibroblasts but not A-T fibroblasts, suggesting it is a specific ATM kinase radiosensitizer [1].
    KU-60019 can reduce radiation-induced S473 AKT phosphorylation in human glioma cell lines that are p53 wild type (U87) and p53 mutant (U1242). However, the suppression of AKT does not enhance radiosensitization of KU-60019 [1].
    KU-60019 has been reported to inhibit cell migration and invasion in human glioma cells U87 and U1242 in a dose-dependent manner. Besides, KU-60019, to some extent, has also been shown to suppress the growth of U1242 cells [1].
    
    [1] Golding SE1, Rosenberg E, Valerie N, Hussaini I, Frigerio M, Cockcroft XF, Chong WY, Hummersone M, Rigoreau L, Menear KA, O'Connor MJ,Povirk LF, van Meter T, Valerie K. Improved ATM kinase inhibitor KU-60019 radiosensitizes glioma cells, compromises insulin, AKT and ERK prosurvival signaling, and inhibits migration and invasion. Mol Cancer Ther. 2009 Oct;8(10):2894-902.
- Properties
  - Alternative Name
    
    KU60019;KU 60019; 2-[(2S,6R)-2,6-dimethylmorpholin-4-yl]-N-[5-(6-morpholin-4-yl-4-oxopyran-2-yl)-9H-thioxanthen-2-yl]acetamide
    
    CAS Number
    
    925701-49-1
    
    Molecular Formula
    
    C30H33N3O5S
    
    Molecular Weight
    
    547.68
    
    Purity
    
    Purity= 99.76%
    
    Solubility
    
    ≥27.4 mg/mL in DMSO; insoluble in H2O; ≥51.2 mg/mL in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Mathew J.K. Jones, Camille Gelot, et al. "Human DDK rescues stalled forks and counteracts checkpoint inhibition at unfired origins to complete DNA replication." Mol Cell. 2021 Feb 4;81(3):426-441.e8. PMID:33545059
    2. Zheng K, Ma J, et al. "Sulforaphane Inhibits Autophagy and Induces Exosome-Mediated Paracrine Senescence via Regulating mTOR/TFE3." Mol Nutr Food Res. 2020;e1901231. PMID:32476238
    3. Zhao K, Wang X, et al. "A long noncoding RNA sensitizes genotoxic treatment by attenuating ATM activation and homologous recombination repair in cancers." PLoS Biol. 2020;18(3):e3000666. PMID:32203529
    4. Christine Wenz. "Cell confluence as crucial regulator of ROS-induced toxicity: Analysis of t-BuOOH-induced cell death in vitro." Gutenberg-Universität in Mainz. 2019.
    5. Caster JM, Yu SK, et al. "Effect of particle size on the biodistribution, toxicity, and efficacy of drug-loaded polymeric nanoparticles in chemoradiotherapy." Nanomedicine. 2017 Mar 11. pii: S1549-9634(17)30044-8. PMID:28300658
    6. Mignon Albertha van Vuuren. "The role of Atm in the regulation of cardiomyocyte glucose utilization under normal and insulin resistant conditions." Stellenbosch University. March 2016.

KU-60019

Background

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