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HomeProduct name listKU-55933

KU-55933

KU-55933 Structural

What is KU-55933?

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

The Uses of KU-55933

KU-55933 has been used as an ataxia-telangiectasia mutated (Atm) inhibitor.

The Uses of KU-55933

A potent and specific ATM kinase inhibitor with an IC50 and a Ki of 13 nM and 2.2 nM, respectively.

What are the applications of Application

ATM Kinase Inhibitor is a cell-permeable, potent, selective and ATP-competitive ATM inhibitor

Definition

ChEBI: 2-(4-morpholinyl)-6-(1-thianthrenyl)-4-pyranone is a thianthrene.

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.

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

Properties of KU-55933

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)
pka 0.33±0.20(Predicted)
form  powder
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.

Safety information for KU-55933

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for KU-55933

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