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Submit ReviewKU 55933
Description: Potent and selective ATM kinase inhibitor
Chemical Name: 2-(4-Morpholinyl)-6-(1-thianthrenyl)-4H-pyran-4-one
Purity: ≥98% (HPLC)
Biological Activity for KU 55933
KU 55933 is a potent, 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.
Technical Data for KU 55933
| M. Wt | 395.49 |
| Formula | C21H17NO3S2 |
| Storage | Desiccate at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 587871-26-9 |
| PubChem ID | 5278396 |
| InChI Key | XRKYMMUGXMWDAO-UHFFFAOYSA-N |
| Smiles | O=C1C=C(C3=CC=CC4=C3SC5=C(C=CC=C5)S4)OC(N2CCOCC2)=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for KU 55933
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 39.55 | 100 | |
| ethanol | 19.77 | 50 |
Preparing Stock Solutions for KU 55933
The following data is based on the product molecular weight 395.49. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.53 mL | 12.64 mL | 25.29 mL |
| 5 mM | 0.51 mL | 2.53 mL | 5.06 mL |
| 10 mM | 0.25 mL | 1.26 mL | 2.53 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.51 mL |
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Product Datasheets for KU 55933
References for KU 55933
References are publications that support the biological activity of the product.
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
Eaton et al (2007) Ataxia-telangiectasia mutated kinase regulates ribonucleotide reductase and mitochondrial homeostasis. J.Clin.Invest. 117 2723 PMID: 17786248
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
If you know of a relevant reference for KU 55933, please let us know.
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Keywords: KU 55933, KU 55933 supplier, Potent, selective, ATM, kinase, inhibitors, inhibits, Ataxia, Telangiectasia, Mutated, Kinase, Kinases, KU55933, &, ATR, Checkpoint, Control, 3544, Tocris Bioscience
97 Citations for KU 55933
Citations are publications that use Tocris products. Selected citations for KU 55933 include:
Regina et al (2022) Dual signaling via interferon and DNA damage response elicits entrapment by giant PML nuclear bodies. Elife 11 PMID: 35319461
Jennifer A et al (2022) High replication stress and limited Rad51-mediated DNA repair capacity, but not oxidative stress, underlie oligodendrocyte precursor cell radiosensitivity. NAR Cancer 4 zcac012 PMID: 35425901
Xia et al (2022) Citrate Promotes Excessive Lipid Biosynthesis and Senescence in Tumor Cells for Tumor Therapy. Adv Sci (Weinh) 9 e2101553 PMID: 34747157
Rosina et al (2019) Osteogenic differentiation of skeletal muscle progenitor cells is activated by the DNA damage response. Sci Rep 9 5447 PMID: 30931986
Calo et al (2018) Tissue-selective effects of nucleolar stress and rDNA damage in developmental disorders. Nature 554 112 PMID: 29364875
Acebes-Huerta et al (2016) Drug-induced hyperploidy stimulates an antitumor NK cell response mediated by NKG2D and DNAM-1 receptors. Oncoimmunology 5 e1074378 PMID: 27057443
Langlands et al (2016) Fe65 Is Phosphorylated on Ser289 after UV-Induced DNA Damage. PLoS One 11 e0155056 PMID: 27176072
Majid et al (2014) PARP-1 dependent recruitment of the amyotrophic lateral sclerosis-associated protein FUS/TLS to sites of oxidative DNA damage. Nucleic Acids Res 42 307-14 PMID: 24049082
Satish et al (2014) N-nitroso-N-ethylurea activates DNA damage surveillance pathways and induces transformation in mammalian cells. BMC Cancer 14 287 PMID: 24758542
Alberto et al (2014) Inactivation of p53 in Human Keratinocytes Leads to Squamous Differentiation and Shedding via Replication Stress and Mitotic Slippage. Cell Rep 9 1349-60 PMID: 25453755
Ronald et al (2013) Repair of DNA strand breaks in a minichromosome in vivo: kinetics, modeling, and effects of inhibitors. PLoS One 8 e52966 PMID: 23382828
Alberto et al (2019) E3 Ubiquitin Ligases RNF20 and RNF40 Are Required for Double-Stranded Break (DSB) Repair: Evidence for Monoubiquitination of Histone H2B Lysine 120 as a Novel Axis of DSB Signaling and Repair. Mol Cell Biol 39 PMID: 30692271
So-Youn et al (2019) Transient inhibition of p53 homologs protects ovarian function from two distinct apoptotic pathways triggered by anticancer therapies. Cell Death Differ 26 502-515 PMID: 29988075
Kenneth M et al (2019) RAG-Mediated DNA Breaks Attenuate PU.1 Activity in Early B Cells through Activation of a SPIC-BCLAF1 Complex. Cell Rep 29 829-843.e5 PMID: 31644907
Russell M et al (2019) Autophagy is essential for oligodendrocyte differentiation, survival, and proper myelination. Glia 67 1745-1759 PMID: 31162728
Piquet et al (2018) The Histone Chaperone FACT Coordinates H2A.X-Dependent Signaling and Repair of DNA Damage. Mol Cell 72 888 PMID: 30344095
Wu et al (2014) Selenoprotein H suppresses cellular senescence through genome maintenance and redox regulation. J Biol Chem 289 34378 PMID: 25336634
Sakai et al (2014) Wild-type p53-induced phosphatase 1 (Wip1) forestalls cellular premature senescence at physiological oxygen levels by regulating DNA damage response signaling during DNA replication. Cell Cycle 13 1015 PMID: 24552809
Kim and Suh (2014) Defying DNA double-strand break-induced death during prophase I meiosis by temporal TAp63α phosphorylation regulation in developing mouse oocytes. Mol Cell Biol 34 1460 PMID: 24515437
Alekseev et al (2014) Inhibition of ataxia telangiectasia mutated (ATM) kinase suppresses herpes simplex virus type 1 (HSV-1) keratitis. Invest Ophthalmol Vis Sci 55 706 PMID: 24370835
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
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
Yamamoto et al (2012) Kinase-dead ATM protein causes genomic instability and early embryonic lethality in mice. J Virol 198 305 PMID: 22869596
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
Tarek et al (2020) A robust CRISPR-Cas9-based fluorescent reporter assay for the detection and quantification of DNA double-strand break repair. Nucleic Acids Res 48 e126 PMID: 33068408
Lambrus et al (2016) A USP28-53BP1-p53-p21 signaling axis arrests growth after centrosome loss or prolonged mitosis. J Cell Biol 214 143 PMID: 27432896
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
Gibbs-Seymour et al (2015) Lamin A/C-dependent interaction with 53BP1 promotes cellular responses to DNA damage. Open Biol 14 162 PMID: 25645366
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
Hollingworth et al (2015) Activation of DNA Damage Response Pathways during Lytic Replication of KSHV. Mol Cell Biol 7 2908 PMID: 26057167
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
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
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
Alvarez-Quilón et al (2014) ATM specifically mediates repair of double-strand breaks with blocked DNA ends. Nat Commun 5 3347 PMID: 24572510
Ye et al (2014) TLR8 signaling enhances tumor immunity by preventing tumor-induced T-cell senescence. EMBO Mol Med 6 1294 PMID: 25231413
Chaudhary et al (2014) SMAR1 coordinates HDAC6-induced deacetylation of Ku70 and dictates cell fate upon irradiation. Cell Death Dis 5 e1447 PMID: 25299772
Edwards et al (2018) The ATM and Rad3-Related (ATR) Protein Kinase Pathway Is Activated by Herpes Simplex Virus 1 and Required for Efficient Viral Replication. J Virol 92 PMID: 29263259
Delgado-Benito et al (2018) The Chromatin Reader ZMYND8 Regulates Igh Enhancers to Promote Immunoglobulin Class Switch Recombination. Mol Cell 72 636 PMID: 30293785
Gautam et al (2018) SETD2-dependent H3K36me3 plays a critical role in epigenetic regulation of the HPV31 life cycle. PLoS Pathog 14 e1007367 PMID: 30312361
Bhatia et al (2018) Formation of 53BP1 foci and ATM activation under oxidative stress is facilitated by RNA:DNA hybrids and loss of ATM-53BP1 expression promotes photoreceptor cell survival in mice. F1000Res 7 1233 PMID: 30345028
Yang et al (2018) Cell type-dependent bimodal p53 activation engenders a dynamic mechanism of chemoresistance. Sci Adv 4 eaat5077 PMID: 30585287
Jaiswal et al (2017) ATM/Wip1 activities at chromatin control Plk1 re-activation to determine G2 checkpoint duration. EMBO J 36 2161 PMID: 28607002
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
Balmus et al (2019) ATM orchestrates the DNA-damage response to counter toxic non-homologous end-joining at broken replication forks. Nat Commun 10 87 PMID: 30622252
Moore et al (2019) The CHD6 chromatin remodeler is an oxidative DNA damage response factor. Nat Commun 10 241 PMID: 30651562
Wu et al (2017) NOX2-dependent ATM kinase activation dictates pro-inflammatory macrophage phenotype and improves effectiveness to radiation therapy. Cell Death Differ 24 1632 PMID: 28574504
Okita et al (2015) Contrasting Effects of the Cytotoxic Anticancer Drug gemcit. and the EGFR Tyrosine Kinase Inhibitor gefi. on NK Cell-Mediated Cytotoxicity via Regulation of NKG2D Ligand in Non-Small-Cell Lung Cancer Cells. PLoS One 10 e0139809 PMID: 26439264
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
Sheng et al (2014) Preconditioning stimuli induce autophagy via sphingosine kinase 2 in mouse cortical neurons. Oncotarget 289 20845 PMID: 24928515
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
Bothmer et al (2013) Mechanism of DNA resection during intrachromosomal recombination and immunoglobulin class switching. Chembiochem 210 115 PMID: 23254285
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
Luo et al (2011) Parvovirus B19 infection of human primary erythroid progenitor cells triggers ATR-Chk1 signaling, which promotes B19 virus replication. J Virol 85 8046 PMID: 21680529
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
Vázquez-Cedeira et al (2011) Differential inhibitor sensitivity between human kinases VRK1 and VRK2. PLoS One 6 e23235 PMID: 21829721
Farkas et al (2011) Identification of small molecule inhibitors of phosphatidylinositol 3-kinase and autophagy. J Biol Chem 286 38904 PMID: 21930714
Paul et al (2019) Protein Phosphatase 1 Regulatory Subunit SDS22 Inhibits Breast Cancer Cell Tumorigenesis by Functioning as a Negative Regulator of the AKT Signaling Pathway. Neoplasia 21 30 PMID: 30500680
Peidis et al (2011) Doxorubicin bypasses the cytoprotective effects of eIF2α phosphorylation and promotes PKR-mediated cell death. Cell Death Differ 18 145 PMID: 20559319
Helmink et al (2011) H2AX prevents CtIP-mediated DNA end resection and aberrant repair in G1-phase lymphocytes. Nature 469 245 PMID: 21160476
Bagamanshina et al (2019) Cytotoxic and Antitumor Activity of Lactaptin in Combination with Autophagy Inducers and Inhibitors. Biomed Res Int 2019 4087160 PMID: 31317028
Yeganeh et al (2019) Autophagy is required for lung development and morphogenesis. J Clin Invest 130 2904 PMID: 31162135
Benkafadar et al (2017) Reversible p53 inhibition prevents cisplatin ototoxicity without blocking chemotherapeutic efficacy. EMBO Mol Med 9 7 PMID: 27794029
Allen et al (2015) DNA Damage Response Proteins and Oxygen Modulate Prostaglandin E2 Growth Factor Release in Response to Low and High LET Ionizing Radiation. Front Oncol 5 260 PMID: 26697402
Ahmed et al (2015) Selective Inhibition of Parallel DNA Damage Response Pathways Optimizes Radiosensitization of Glioblastoma Stem-like Cells. Cancer Res 75 4416 PMID: 26282173
Rodgers et al (2015) Spatio-temporal regulation of RAG2 following genotoxic stress. DNA Repair (Amst) 27 19 PMID: 25625798
Beggs et al (2015) Trovafloxacin-induced replication stress sensitizes HepG2 cells to tumor necrosis factor-alpha-induced cytotoxicity mediated by extracellular signal-regulated kinase and ataxia telangiectasia and Rad3-related. Toxicology 331 35 PMID: 25748550
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
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
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
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
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
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
Kanai et al (2012) Oncolytic virus-mediated manipulation of DNA damage responses: synergy with chemotherapy in killing glioblastoma stem cells. J Natl Cancer Inst 104 42 PMID: 22173583
Sultana et al (2012) Synthetic lethal targeting of DNA double-strand break repair deficient cells by human apurinic/apyrimidinic endonuclease inhibitors. Int J Cancer 131 2433 PMID: 22377908
Kumar et al (2012) Role for Rif1 in the checkpoint response to damaged DNA in Xenopus egg extracts. Cell Cycle 11 1183 PMID: 22391207
Ando et al (2012) PIDD death-domain phosphorylation by ATM controls prodeath versus prosurvival PIDDosome signaling. Mol Cell 47 681 PMID: 22854598
Alan et al (2012) Preclinical development of the novel Chk1 inhibitor SCH900776 in combination with DNA-damaging agents and antimetabolites. Mol Cancer Ther 11 427-38 PMID: 22203733
H et al (2011) Abrogation of Wip1 expression by RITA-activated p53 potentiates apoptosis induction via activation of ATM and inhibition of HdmX. Cell Death Differ 18 1736-45 PMID: 21546907
Anthony D et al (2011) An ataxia-telangiectasia-mutated (ATM) kinase mediated response to DNA damage down-regulates the mRNA-binding potential of THOC5. RNA 17 1957-66 PMID: 21937706
John et al (2021) HCV Activates Somatic L1 Retrotransposition-A Potential Hepatocarcinogenesis Pathway. Cancers (Basel) 13 PMID: 34680227
Ibler et al (2019) Typhoid toxin exhausts the RPA response to DNA replication stress driving senescence and Salmonella infection. Nat Commun 10 4040 PMID: 31492859
Thomas A et al (2018) Dppa2/4 Facilitate Epigenetic Remodeling during Reprogramming to Pluripotency. Cell Stem Cell 23 396-411.e8 PMID: 30146411
Jingwen et al (2017) Nuclear Acetyl-CoA Production by ACLY Promotes Homologous Recombination. Mol Cell 67 252-265.e6 PMID: 28689661
Dale A et al (2017) Regulation of human polλ by ATM-mediated phosphorylation during non-homologous end joining. DNA Repair (Amst) 51 31-45 PMID: 28109743
Sultana et al (2013) Targeting XRCC1 deficiency in breast cancer for personalized therapy. Cancer Res 73 1621 PMID: 23253910
Passaro et al (2013) Ionizing radiation enhances dl922-947-mediated cell death of anaplastic thyroid carcinoma cells. Endocr Relat Cancer 20 633 PMID: 23839822
Valero et al (2013) E1a promotes c-Myc-dependent replicative stress: implications in glioblastoma radiosensitization. Cell Cycle 13 52 PMID: 24196438
Luo et al (2013) SMC1-mediated intra-S-phase arrest facilitates bocavirus DNA replication. J Virol 87 4017 PMID: 23365434
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
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
Fumagalli et al (2012) Telomeric DNA damage is irreparable and causes persistent DNA-damage-response activation. Nat Cell Biol 14 355 PMID: 22426077
Yuan et al (2012) Regulation of SIRT1 activity by genotoxic stress. Genes Dev 26 791 PMID: 22465953
Neumayer et al (2012) Targeting protein for xenopus kinesin-like protein 2 (TPX2) regulates γ-histone 2AX (γ-H2AX) levels upon ionizing radiation. J Biol Chem 287 42206 PMID: 23045526
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
Michael T et al (2010) DNA damage-mediated induction of a chemoresistant niche. Cell 143 355-66 PMID: 21029859
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Reviews for KU 55933
Average Rating: 5 (Based on 2 Reviews.)
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Filter by:
ATM inhibitor.
By
Isabelle Cristine da Costa on 09/23/2021
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: U2OS
I used this ATM inhibitor (ATMi - KU55933) to treat human osteosarcoma cells and then I blotted for pATM (S1981) and for pCHK2 (T68) to assess ATM inhibition. It works incredibly well!
Inhibition of ATM results in DNA damage.
By
Anonymous on 02/29/2020
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: Hela
HeLa cells transfected with in vitro transcribed I-PpoI and treated or not with inhibitors for KU 55933 and NU 7441 (iDPK)
Literature in this Area
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Cell Cycle and DNA Damage Research Product Guide
This product guide provides a review of the cell cycle and DNA damage research area and lists over 150 products, including research tools for:
- Cell Cycle and Mitosis
- DNA Damage Repair
- Targeted Protein Degradation
- Ubiquitin Proteasome Pathway
- Chemotherapy Targets
Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.