Cat. No. 3544
Chemical Name: 2-(4-Morpholinyl)-6-(1-thianthrenyl
Biological ActivityPotent, selective and competitive ATM kinase inhibitor (Ki = 2.2 nM, IC50 values are 13, 2500, 9300, 16600, > 100000 and > 100000 nM at ATM, DNA-PK, mTOR, PI 3-kinase, PI 4-K and ATR respectively). Decreases viability of MCF-7, A549 and HCT116 cells and decreases p21CIP1 levels in vitro. Acts as a radio- and chemosensitizer for the treatment of cancer.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Safety Data Sheet
Crescenzi et al (2008) Ataxia telangiectasia mutated and p21CIP1 modulate cell survival of drug-induced senescent tumor cells: implications for chemotherapy. Clin.Cancer Res. 14 1877. PMID: 18347191.
Eaton et al (2007) Ataxia-telangiectasia mutated kinase regulates ribonucleotide reductase and mitochondrial homeostasis. J.Clin.Invest. 117 2723. PMID: 17786248.
Hickson et al (2004) Identification and characterization of a novel and specific inhibitor of the ataxia-telangiectasia mutated kinase ATM. Cancer Res. 64 9152. PMID: 15604286.
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Citations are publications that use Tocris products. Selected citations for KU 55933 include:
Colin et al (2015) Cellular responses to a prolonged delay in mitosis are determined by a DNA damage response controlled by Bcl-2 family proteins. Viruses 5 140156. PMID: 25761368.
Gibbs-Seymour et al (2015) Lamin A/C-dependent interaction with 53BP1 promotes cellular responses to DNA damage. Open Biol 14 162. PMID: 25645366.
Hollingworth et al (2015) Activation of DNA Damage Response Pathways during Lytic Replication of KSHV. Mol Cell Biol 7 2908. PMID: 26057167.
Liu et al (2015) A radiosensitivity MiRNA signature validated by the TCGA database for head and neck squamous cell carcinomas. Aging Cell 6 34649. PMID: 26452218.
Malonia et al (2015) F-box protein FBXO31 directs degradation of MDM2 to facilitate p53-mediated growth arrest following genotoxic stress. J Cell Biol 112 8632. PMID: 26124108.
Okita et al (2015) Contrasting Effects of the Cytotoxic Anticancer Drug Gemcitabine and the EGFR Tyrosine Kinase Inhibitor Gefitinib on NK Cell-Mediated Cytotoxicity via Regulation of NKG2D Ligand in Non-Small-Cell Lung Cancer Cells. PLoS One 10 e0139809. PMID: 26439264.
Stechow et al (2015) The E3 ubiquitin ligase ARIH1 protects against genotoxic stress by initiating a 4EHP-mediated mRNA translation arrest. Proc Natl Acad Sci U S A 35 1254. PMID: 25624349.
Teng et al (2015) Pharmacologic inhibition of ATR and ATM offers clinically important distinctions to enhancing platinum or radiation response in ovarian, endometrial, and cervical cancer cells. Gynecol Oncol 136 554. PMID: 25560806.
Alvarez-Quilón et al (2014) ATM specifically mediates repair of double-strand breaks with blocked DNA ends. Nat Commun 5 3347. PMID: 24572510.
Chaudhary et al (2014) SMAR1 coordinates HDAC6-induced deacetylation of Ku70 and dictates cell fate upon irradiation. Cell Death Dis 5 e1447. PMID: 25299772.
Henriksson et al (2014) The scaffold protein WRAP53β orchestrates the ubiquitin response critical for DNA double-strand break repair. Genes Dev 28 2726. PMID: 25512560.
Sheng et al (2014) Preconditioning stimuli induce autophagy via sphingosine kinase 2 in mouse cortical neurons. Oncotarget 289 20845. PMID: 24928515.
Ye et al (2014) TLR8 signaling enhances tumor immunity by preventing tumor-induced T-cell senescence. EMBO Mol Med 6 1294. PMID: 25231413.
Bothmer et al (2013) Mechanism of DNA resection during intrachromosomal recombination and immunoglobulin class switching. Chembiochem 210 115. PMID: 23254285.
Britton et al (2013) A new method for high-resolution imaging of Ku foci to decipher mechanisms of DNA double-strand break repair. J Cell Biol 202 579. PMID: 23897892.
Cataldi and McCarty (2013) Hairpin-end conformation of adeno-associated virus genome determines interactions with DNA-repair pathways. J Biol Chem 20 686. PMID: 23151519.
Edwards et al (2013) Human papillomavirus episome stability is reduced by aphidicolin and controlled by DNA damage response pathways. J Virol 87 3979. PMID: 23365423.
Fard et al (2013) The heterogenic final cell cycle of chicken retinal Lim1 horizontal cells is not regulated by the DNA damage response pathway. Cell Cycle 13 408. PMID: 24247150.
Lee et al (2013) Functional intersection of ATM and DNA-dependent protein kinase catalytic subunit in coding end joining during V(D)J recombination. PLoS One 33 3568. PMID: 23836881.
Lottersberger et al (2013) Role of 53BP1 oligomerization in regulating double-strand break repair. Proc Natl Acad Sci U S A 110 2146. PMID: 23345425.
Montané and Menand (2013) ATP-competitive mTOR kinase inhibitors delay plant growth by triggering early differentiation of meristematic cells but no developmental patterning change. Nat Chem Biol 64 4361. PMID: 23963679.
Oksenych et al (2013) Functional redundancy between the XLF and DNA-PKcs DNA repair factors in V(D)J recombination and nonhomologous DNA end joining. J Biol Chem 110 2234. PMID: 23345432.
Yüce and West (2013) Senataxin, defective in the neurodegenerative disorder ataxia with oculomotor apraxia 2, lies at the interface of transcription and the DNA damage response. Mol Cell Biol 33 406. PMID: 23149945.
Fumagalli et al (2012) Telomeric DNA damage is irreparable and causes persistent DNA-damage-response activation. Nat Cell Biol 14 355. PMID: 22426077.
Klotz-Noack et al (2012) Re-replication induced by geminin depletion occurs from G2 and is enhanced by checkpoint activation. J Cell Sci 125 2436. PMID: 22366459.
Mund et al (2012) SPOC1 modulates DNA repair by regulating key determinants of chromatin compaction and DNA damage response. Nucleic Acids Res 40 11363. PMID: 23034801.
Richardson et al (2012) Mechanism-based screen establishes signalling framework for DNA damage-associated G1 checkpoint response. PLoS One 7 e31627. PMID: 22384045.
Sullivan et al (2012) ATM and MET kinases are synthetic lethal with nongenotoxic activation of p53. Proc Natl Acad Sci U S A 8 646. PMID: 22660439.
Tang et al (2012) Detection of early Abl kinase activation after ionizing radiation by using a peptide biosensor. Mol Cell Biol 13 665. PMID: 22334513.
Yamamoto et al (2012) Kinase-dead ATM protein causes genomic instability and early embryonic lethality in mice. J Virol 198 305. PMID: 22869596.
Yuan et al (2012) Regulation of SIRT1 activity by genotoxic stress. Genes Dev 26 791. PMID: 22465953.
Farkas et al (2011) Identification of small molecule inhibitors of phosphatidylinositol 3-kinase and autophagy. J Biol Chem 286 38904. PMID: 21930714.
Sharma et al (2011) γ-Radiation promotes immunological recognition of cancer cells through increased expression of cancer-testis antigens in vitro and in vivo. Gene Ther 6 e28217. PMID: 22140550.
Vázquez-Cedeira et al (2011) Differential inhibitor sensitivity between human kinases VRK1 and VRK2. PLoS One 6 e23235. PMID: 21829721.
Yin and Glass (2011) The phenotypic radiation resistance of CD44+/CD24(-or low) breast cancer cells is mediated through the enhanced activation of ATM signaling. PLoS One 6 e24080. PMID: 21935375.
Cataldi and McCarty (2010) Differential effects of DNA double-strand break repair pathways on single-strand and self-complementary adeno-associated virus vector genomes. J Exp Med 84 8673. PMID: 20538857.
Qi et al (2010) Selenium compounds activate ATM-dependent DNA damage response via the mismatch repair protein hMLH1 in colorectal cancer cells. Am J Physiol Cell Physiol 285 33010. PMID: 20709753.
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Keywords: KU 55933, supplier, Potent, selective, ATM, kinase, inhibitors, inhibits, Ataxia, Telangiectasia, Mutated, Kinase, Kinases, KU55933, Tocris Bioscience, ATM and ATR Kinase Inhibitor products
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