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| KU-55933 Basic information |
| Product Name: | KU-55933 | | Synonyms: | 2-MORPHOLIN-4-YL-6-THIANTHREN-1-YL-PYRAN-4-ONE;2-(4-Morpholinyl)-6-(1-thianthrenyl)-4H-pyran-4-one;KU-55933 (ATM Kinase Inhibitor);KU-55933, >99%;KV-55933;2-morpholino-6-(thianthren-1-yl)-4H-pyran-4-one;2-Morpholin-4-yl-6-thianthren-1-ylpyran-4-one KU-55933 (ATM Kinase Inhibitor);KU 55933, >=98% | | CAS: | 587871-26-9 | | MF: | C21H17NO3S2 | | MW: | 395.49 | | EINECS: | | Product Categories: | Inhibitors | | Mol File: | 587871-26-9.mol |
| KU-55933 Chemical Properties |
| Boiling point | 628.0±55.0 °C(Predicted) | | density | 1.419±0.06 g/cm3(Predicted) | | storage temp. | -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. |
| KU-55933 Usage And Synthesis |
| 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. | | Uses | KU-55933 has been used as an ataxia-telangiectasia mutated (Atm) inhibitor. | | 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. | | 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. | | 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 |
| KU-55933 Preparation Products And Raw materials |
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