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KU60019

Catalog No. T2474 CAS 925701-49-1

Synonyms: KU-60019, KU 60019

Ku-60019 is a potent, reversible inhibitor of ATM kinase (IC50: 6.3 nM). It is much less effective or without effect against a panel of 229 other kinases.

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KU60019, CAS 925701-49-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 48.00
5 mg	In stock	$ 108.00
10 mg	In stock	$ 153.00
25 mg	In stock	$ 298.00
50 mg	In stock	$ 442.00
1 mL * 10 mM (in DMSO)	In stock	$ 142.00

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Purity: 99.14%

ee: 100%

Purity: 98.79%

ee: 100%

Purity: 98%

Purity: 95.9%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Ku-60019 is a potent, reversible inhibitor of ATM kinase (IC50: 6.3 nM). It is much less effective or without effect against a panel of 229 other kinases.
Targets&IC50	ATM:6.3 nM (cell free)
In vitro	KU-60019 is an improved inhibitor of the ATM kinase with an IC50 of 6.3 nM, approximately half that of KU-55933. The IC50 values for DNA-PKcs and ATR are 1.7 and >10 μM, respectively, almost 270-and 1600-fold higher than for ATM [1]. KU-60019 at 300 nM completely inhibited p53 and H2AX phosphorylation as quickly as 15 min after application. When U1242 cells were treated with KU-60019 for 1 h, washed to remove KU-60019 and then challenged with IR, the inhibitory effects of KU-60019 were reversed as early as 15 min after washout [2].
In vivo	Despite PTEN-deficient control tumors reaching a 4-fold increase in size before PTEN wild-type controls, KU-60019–treated PTEN-deficient tumors displayed a statistically significant slowing in growth. This growth inhibition was especially evident at the start of the experiment (days 5–12) just after KU-60019 was administered (days 1–5) [3]. When mice harboring U1242/luc-GFP tumors were treated with KU-60019 administered from an osmotic pump followed by 2 Gy of irradiation, we were able to demonstrate a complete elimination of tumor cells on day 20 by bioluminescence imaging (BLI) 7 days after radiation [4].
Cell Research	Cell growth was determined by AlamarBlue. U1242 cells were serially diluted, allowed to attach for 6 h and then exposed to KU-60019 at 3 μM. At days 1, 3 and 5 after seeding, AlamarBlue was added to the medium to the recommended final concentration. Plates were incubated for 1 h at 37°C and fluorescence determined on a FluoroCount plate reader (excitation 530 nm, emission 590 nm) and values taken as a measure of cell growth [1].
Animal Research	Cells (3 × 10^7) were implanted into male Fox Chase Severe Combined Immunodeficiency (SCID) mice. Administration of doxycycline was started when tumors reached 100 mm3 in volume and was performed every 48 hours up to removal of the animal from the experiment. Forty-eight hours after PTEN induction, animals were administered KU-60019 (100 mg/kg) for 5 consecutive days and measured until they reached a target 400 mm3 volume. Measurements of tumor volume and body weight took place every 3 days using calipers [3].

Synonyms	KU-60019, KU 60019
Molecular Weight	547.67
Formula	C30H33N3O5S
CAS No.	925701-49-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 15 mg/mL (27.4 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Golding SE, et al. Improved ATM kinase inhibitor KU-60019 radiosensitizes glioma cells, compromises insulin, AKT and ERK prosurvival signaling, and inhibits migration and invasion. Mol Cancer Ther. 2009 Oct;8(10):2894-902. 2. Golding SE, et al. Dynamic inhibition of ATM kinase provides a strategy for glioblastoma multiforme radiosensitization and growth control. Cell Cycle. 2012 Mar 15;11(6):1167-73. 3. McCabe N, et al. Mechanistic Rationale to Target PTEN-Deficient Tumor Cells with Inhibitors of the DNA Damage Response Kinase ATM. Cancer Res. 2015 Jun 1;75(11):2159-65. 4. Biddlestone-Thorpe L, et al. ATM kinase inhibition preferentially sensitizes p53-mutant glioma to ionizing radiation. Clin Cancer Res. 2013 Jun 15;19(12):3189-200. 5. Liang J, Niu Z, Yu X, et al. Counteracting Genome Instability by p53-dependent Mintosis[J]. bioRxiv. 2020. 6. Liang J, Niu Z, Zhang B, et al. Liang J, Niu Z, Zhang B, et al. p53-dependent elimination of aneuploid mitotic offspring by entosis[J]. Cell Death & Differentiation. 2020: 1-15. 7. Ha G H, Ji J H, Chae S, et al. Pellino1 regulates reversible ATM activation via NBS1 ubiquitination at DNA double-strand breaks[J]. Nature communications. 2019 Apr 5;10(1):1577.

Citations

1. Ha G H, Ji J H, Chae S, et al. Pellino1 regulates reversible ATM activation via NBS1 ubiquitination at DNA double-strand breaks. Nature communications. 2019 Apr 5;10(1):1577. 2. Liang J, Niu Z, Zhang B, et al. p53-dependent elimination of aneuploid mitotic offspring by entosis. Cell Death & Differentiation. 2020: 1-15 3. Liang J, Niu Z, Zhang B, et al Liang J, Niu Z, Zhang B, et al. p53-dependent elimination of aneuploid mitotic offspring by entosis. Cell Death & Differentiation. 2020: 1-15. 4. Qiao S, Lu W, Glorieux C, et al. Wild-type IDH2 protects nuclear DNA from oxidative damage and is a potential therapeutic target in colorectal cancer. Oncogene. 2021: 1-13.

Related compound libraries

This product is contained In the following compound libraries：

Tyrosine Kinase Inhibitor Library Neural Regeneration Compound Library Reprogramming Compound Library Cancer Cell Differentiation Compound Library HIF-1 Signaling Pathway Compound Library Oxidation-Reduction Compound Library PI3K-AKT-mTOR Compound Library Kinase Inhibitor Library NO PAINS Compound Library Target-Focused Phenotypic Screening Library

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Keywords

KU60019 925701-49-1 DNA Damage/DNA Repair PI3K/Akt/mTOR signaling ATM/ATR KU-60019 KU 60019 inhibitor inhibit

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