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KU-55933

Cat. No. M1801
KU-55933 Structure
Synonym:

KU55933

Size Price Availability Quantity
10mg USD 80 In stock
50mg USD 220 In stock
100mg USD 380 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

KU-55933 is a cell-permeable, potent, selective and ATP-competitive inhibitor of ATM (Ataxia telangiectasia mutated), a serine/threonine protein kinase, that exhibits an IC50 of 13 nmol/L and a Ki of 2.2 nmol/L. KU-55933 shows specificity with respect to inhibition of other phosphatidylinositol 3'-kinase-like kinases. Cellular inhibition of ATM by KU-55933 was demonstrated by the ablation of ionizing radiation-dependent phosphorylation of a range of ATM targets, including p53, gammaH2AX, NBS1, and SMC1. KU-55933 did not show inhibition of UV light DNA damage induced cellular phosphorylation events. Exposure of cells to KU-55933 resulted in a significant sensitization to the cytotoxic effects of ionizing radiation and to the DNA double-strand break-inducing chemotherapeutic agents, etoposide, doxorubicin, and camptothecin. Inhibition of ATM by KU-55933 also caused a loss of ionizing radiation-induced cell cycle arrest. By contrast, KU-55933 did not potentiate the cytotoxic effects of ionizing radiation on ataxia-telangiectasia cells, nor did it affect their cell cycle profile after DNA damage. We conclude that KU-55933 is a novel, specific, and potent inhibitor of the ATM kinase.

Protocol
Cell Experiment
Cell lines LU1205 and WM35 cells
Preparation method Apoptosis studies. Cells were exposed to soluble TRAIL (50 ng/mL) alone or in combination with cycloheximide (2 μg/mL). Different variants of combined treatment were used, including γ-irradiation (5 Gy), in the presence or absence of specific inhibitors of signaling pathways followed by TRAIL treatment. Apoptosis was then assessed by quantifying the percentage of hypodiploid nuclei using fluorescence-activated cell sorting analysis.
Concentrations 10 μM
Incubation time 48 h
Animal Experiment
Animal models LU1205 cells Human melanoma transplant in nude mice.
Formulation DMSO
Dosages 10 μM
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 395.49
Formula C21H17NO3S2
CAS Number 587871-26-9
Purity >99%
Solubility DMSO
Storage at -20°C
References

Inhibition of ataxia telangiectasia mutated kinase activity enhances TRAIL-mediated apoptosis in human melanoma cells.
Ivanov VN, et al. Cancer Res. 2009 Apr 15;69(8):3510-9. PMID: 19351839.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: KU-55933, KU55933 supplier, ATM/ATR, inhibitors

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