KU-60019 is a potent ATM kinase inhibitor with IC50 of 6.3 nM. KU-60019 exhibits little to no nonspecific target effects, displaying similar target selectivity to KU 55933. KU-60019 inhibited the phosphorylation of the major DNA damage effectors p53, H2AX and KAP1 as well as AKT. 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 has also been shown to Inhibit invasion and migration of human glioma cells in vitro. KU-60019 is 10-fold more effective than KU-55933 at blocking radiation-induced phosphorylation of key ATM targets in human glioma cells. 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.
BMC Biol. 2021 May 20;19(1):108.
Very long intergenic non-coding (vlinc) RNAs directly regulate multiple genes in cis and trans
KU-60019 purchased from AbMole
Nat Commun. 2019 Dec 20;10(1):5799.
Novel approach reveals genomic landscapes of single-strand DNA breaks with nucleotide resolution in human cells.
KU-60019 purchased from AbMole
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Source | Med Sci Monit (2017). Figure 4.KU-60019 |
| Method | Proliferation assay | |
| Cell Lines | PA-SMCs | |
| Concentrations | 0.1 μM, 0.3 μM, 0.5 μM | |
| Incubation Time | 24 h | |
| Results | The results demonstrated that at a concentration of 0.5 μM, KU60019 increased cell growth more noticeably compared with other groups |
| Molecular Weight | 547.67 |
| Formula | C30H33N3O5S |
| CAS Number | 925701-49-1 |
| Solubility (25°C) | DMSO 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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Tuvusertib is a selective and orally active ATR inhibitor that kills tumor cells by preventing the repair of damaged DNA with a Ki value below 1 μΜ. |
| ATR-IN-24
ATR-IN-24 is a ATR inhibitor. |
| ATM Inhibitor-6
ATM inhibitor-6 (A-193) is a selective ATM kinase inhibitor. |
| ATR-IN-21
ATR-IN-21 is a potent ATR inhibitor with an IC50 value of <1000 nM. |
| ATR-IN-23
ATR-IN-23 is a potent and selective ATR inhibitor with an IC50 of 1.5 nM. |
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