KU-60019
Catalog No.S1570
Molecular Weight(MW): 547.67
KU-60019 is an improved analogue of KU-55933, with IC50 of 6.3 nM for ATM in cell-free assays, 270- and 1600-fold more selective for ATM than DNA-PK and ATR,and is a highly effective radiosensitizer.
6 Customer Reviews
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The ATM-dependent Ser15-p53 phosphorylation was monitored by Western blotting. Protein loading levels were monitored by probing for actin.
Brain Pathol, 2012, 22(5): 677-88 . KU-60019 purchased from Selleck.
Relative quantification of stem cell markers (Prom1, Bmi1, CD15, Msi1, Msi2, Nanog, Nestin, Oct4 and Sox2) in control BORRU epidermal growth factor fibroblast growth factor (EGF-FGF) and radiation-survived BORRU after sensitization with KU-60019 [(EGF-FGF) + KU-60019 + 5 Gy]. BORRU under differentiative conditions [fetal calf serum (FCS)] were used as tissue control (DCtref).
Brain Pathol, 2012, 22(5): 677-88 . KU-60019 purchased from Selleck.
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(a,b) Drug synergy experiment in AALE cells with ATM inhibitor (KU60019) and trametinib (40 nM). Displayed is relative cell viability for KU60019 treatment alone and for co-treatment with trametinib. Error bars indicate s.d. (n=3). (b) Deviation from Bliss additivity calculated from experiment in a. Error bars indicate s.d. (n=3).
Nat Commun, 2016, 7:13701. KU-60019 purchased from Selleck.
C, LN-229 (left) or S-24 (right) cells were treated with KU-60019 or DMSO 4 hours prior to TMZ exposure. Immunofluorescence images were acquired following pATMSer1981 staining (red). Nuclei are stained with DAPI (blue).
Clin Cancer Res, 2018, 24(4):882-895. KU-60019 purchased from Selleck.
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Brain Pathol 2012 22(5), 677-88. KU-60019 purchased from Selleck.
Exp Cell Res, 2018, 366(1):24-33. KU-60019 purchased from Selleck.
Purity & Quality Control
Choose Selective ATM/ATR Inhibitors
Biological Activity
| Description | KU-60019 is an improved analogue of KU-55933, with IC50 of 6.3 nM for ATM in cell-free assays, 270- and 1600-fold more selective for ATM than DNA-PK and ATR,and is a highly effective radiosensitizer. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Features | Improved analog of KU-55933, and is more effective at blocking ATM-mediated DDR events. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Targets |
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| In vitro |
Compared to KU-55933, KU-60019 is an improved more water-soluble inhibitor of the ATM kinase, while displaying similar target selectivity. KU-60019 has little activity against DNA-PKcs and ATR with IC50 values of 1.7 μM and >10 μM, respectively, as well as 229 other protein kinases such as PI3K, mTOR and mTOR/FKBP12. KU-60019 displays 3- to 10-fold more potency than KU-55933 at blocking radiation-induced phosphorylation of key ATM protein targets such as p53, γ-H2AX, and CHK2, in human glioma U87 and U1242 cells, as 1 μM of KU-60019 significantly induces >70% decrease of p53 (S15) phosphorylation to which extent ~10 μM of KU-55933 is required to achieve. KU-60019 effectively radiosensitizes human glioma cells with dose-enhancement ratio of 1.7 and 4.4 at 1 μM and 10 μM, respectively, and also radiosensitizes the normal fibroblasts but not the A-T fibroblasts. KU-60019 treatment (3 μM) blocks basal and insulin-induced AKT S473 phosphorylation by 70% and ~50%, respectively, and completely reduces radiation-induced AKT phosphorylation below the level of control. The effect of KU-60019 on AKT S473 phosphorylation can be seen in glioma cell lines and normal fibroblasts but not in A-T (h-TERT) cells, and can be significantly blocked by phosphatase inhibitor okadaic acid, suggesting a critical role of ATM kinase in regulating AKT phosphorylation via unknown phosphatase. Consistent with the inhibition of prosurvival AKT signaling, KU-60019 at 3 μM significantly inhibits migration and invasion of human glioma U87 cells by >70% and ~60%, respectively, as well as U1242 cells by >50% and ~60% respectively. [1] |
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| Cell Data |
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| In vivo | In orthotopic glioma U1242/luc-GFP xenograft models, the combination of KU-60019 and radiation significantly increases survival of mice than KU-60019 alone, radiation alone, or no treatment. In addition, p53-mutant gliomas is much more sensitive to KU-60019 radiosensitization than wild-type glioma. [2] |
Protocol
| Cell Research:[1] |
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| Animal Research:[2] |
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Solubility (25°C)
| In vitro | DMSO | 18 mg/mL warmed (32.86 mM) |
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| Water | Insoluble | |
| Ethanol | Insoluble |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 547.67 |
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| Formula | C30H33N3O5S |
| CAS No. | 925701-49-1 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
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