Identification | More | [Name]
KU-55933 (ATM Kinase Inhibitor) | [CAS]
587871-26-9 | [Synonyms]
KV-55933 KU-55933, >99% KU-55933 (ATM Kinase Inhibitor) 2-MORPHOLIN-4-YL-6-THIANTHREN-1-YL-PYRAN-4-ONE 2-morpholino-6-(thianthren-1-yl)-4H-pyran-4-one 2-(4-Morpholinyl)-6-(1-thianthrenyl)-4H-pyran-4-one 2-Morpholin-4-yl-6-thianthren-1-ylpyran-4-one KU-55933 (ATM Kinase Inhibitor) | [Molecular Formula]
C21H17NO3S2 | [MDL Number]
MFCD08276985 | [MOL File]
587871-26-9.mol | [Molecular Weight]
395.49 |
Chemical Properties | Back Directory | [Boiling point ]
628.0±55.0 °C(Predicted) | [density ]
1.419±0.06 g/cm3(Predicted) | [storage temp. ]
Desiccate at-20°C | [solubility ]
Soluble in DMSO (up to 40 mg/ml) or in Ethanol (up to 20 mg/ml) | [form ]
powder | [pka]
0.33±0.20(Predicted) | [color ]
white to beige | [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month. |
Hazard Information | Back Directory | [Usage]
A potent and specific ATM kinase inhibitor with an IC50 and a Ki of 13 nM and 2.2 nM, respectively. | [Biological Activity]
Potent, selective and competitive ATM kinase inhibitor (K i = 2.2 nM, IC 50 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 p21 CIP1 levels in vitro . Acts as a radio-and chemosensitizer for the treatment of cancer. | [Description]
Potent and selective ATM kinase inhibitor IC50s= 13, 2500, 9300, 16600, >100000 and >100000 nM for ATM, DNA-PK, mTOR, PI 3-kinase, PI 4-K and ATR respectively.1Decreases viability of MCF-7, A549 and HCT116 cells and decreases p21CIP1?levels?in vitro.2?Disruption of ATM signaling in primary A-T fibroblasts leads to dysregulation of ribonucleotide reductase and increase resistance to inhibitors of mitochondrial respiration and translation.3?Sensitizes radio-resistant cancer cells.4Provides neuroprotection against H2O2-induced cell damage.5 | [Uses]
A potent and specific ATM kinase inhibitor with an IC50 and a Ki of 13 nM and 2.2 nM, respectively. | [Definition]
ChEBI: 2-(4-morpholinyl)-6-(1-thianthrenyl)-4-pyranone is a thianthrene. | [Biochem/physiol Actions]
KU-55933 is a very potent, specific inhibitor of Ataxia telangiectasia (A-T) mutated (ATM) kinase (IC50 = 13 nM). KU-22933 treatment sensitizes cancer cells to ionizing radiation and cytotoxic drugs. The compound KU-22933 blocks ATM-mediated phosphorylyation of p53, gH2AX, NBS1, and SMC1. | [storage]
Desiccate at -20°C | [References]
1) Hickson?et al.?(2004),?Identification and characterization of a novel and specific inhibitor of the ataxia-telangiectasia mutated kinase ATM; Cancer Res.,?64?9152
2) 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
3) Eaton?et al.?(2007),?Ataxia-telangiectasia mutated kinase regulates ribonucleotide reductase and mitochondrial homeostasis; J. Clin. Invest.,?117?2723
4) Zhang?et al.?(2015)?The ATM inhibitor KU55933 sensitizes radioresistant bladder cancer cells with DAB2IP gene defect; Int. J. Radiat. Biol.,?91?368
5) Chwastek?et al.?(2017)?The ATM kinase inhibitor KU-55933 provides neuroprotection against hydrogen peroxide-induced cell damage via a yH2AX/p-p53/caspase-3-independent mechanism: Inhibition of calpain and cathepsin D; Int. J. Biochem. Cell Biol.?87?38 |
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