Art. -Nr.: HY-12061

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KU-60019

28 Cited Publications

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Based on 28 publication(s) in Google Scholar

KU-60019 is an improved ATM kinase-specific inhibitor with IC₅₀ of 6.3 nM.

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Reinheit: 99.43%
CAS. Nr.: 925701-46-8
Formel: C₃₀H₃₃N₃O₅S
Molecular Weight:547.67

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

KU-60019 Chemical Structure

CAS. Nr.: 925701-46-8

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (28)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

KU-60019 is an improved ATM kinase-specific inhibitor with IC₅₀ of 6.3 nM.

IC₅₀ & Target^[1]

ATM

6.3 nM (IC₅₀)

DNA-PKcs

1.7 μM (IC₅₀)

Alle ATM/ATR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HT-29	IC₅₀	0.149 μM Compound: 2; KU-60019	Inhibition of ATM phosphorylation at Ser-1981 residue in human HT-29 cells incubated for 1 hr followed by X-ray irradiation by Hoechst staining based fluorescence plate reader analysis Inhibition of ATM phosphorylation at Ser-1981 residue in human HT-29 cells incubated for 1 hr followed by X-ray irradiation by Hoechst staining based fluorescence plate reader analysis	[PMID: 27259031]
HT-29	IC₅₀	8.5 μM Compound: 2; KU-60019	Inhibition of ATR in human HT-29 cells assessed as reduction in Chk1 phosphorylation at Ser-345 residue after 60 mins in presence of 4-nitroquinoline-1-oxide by Hoechst 33258 staining based plate reader analysis Inhibition of ATR in human HT-29 cells assessed as reduction in Chk1 phosphorylation at Ser-345 residue after 60 mins in presence of 4-nitroquinoline-1-oxide by Hoechst 33258 staining based plate reader analysis	[PMID: 27259031]
MCF7	IC₅₀	11.9 μM Compound: 2; KU-60019	Antiproliferative activity against human MCF7 cells measured after 2 days by SRB assay Antiproliferative activity against human MCF7 cells measured after 2 days by SRB assay	[PMID: 35231830]
MCF7	IC₅₀	2.8 μM Compound: 2; KU-60019	Antiproliferative activity against human MCF7 cells measured after 6 days by SRB assay Antiproliferative activity against human MCF7 cells measured after 6 days by SRB assay	[PMID: 35231830]
SW480	IC₅₀	13.3 μM Compound: 2; KU-60019	Antiproliferative activity against human SW480 cells measured after 3 days by SRB assay Antiproliferative activity against human SW480 cells measured after 3 days by SRB assay	[PMID: 35231830]
SW480	IC₅₀	3.3 μM Compound: 2; KU-60019	Antiproliferative activity against human SW480 cells measured after 9 days by SRB assay Antiproliferative activity against human SW480 cells measured after 9 days by SRB assay	[PMID: 35231830]

In Vitro

KU-60019 is an improved analogue of KU-55933. KU-55933 has an IC₅₀ of 13 nM and K_i of 2.2 nM in vitro and is highly specific for the ATM kinase using a panel of 60 protein kinases. 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. KU-60019 is 10-fold more effective than KU-55933 at blocking radiation-induced phosphorylation of key ATM targets in human glioma cells. In human U87 glioma cells, KU-55933 completely inhibits phosphorylation of p53 (S15) at 10 μM but not at 3 μM, whereas γ-H2AX levels are only partly reduced with 10 μM 1 h after irradiation. By comparison, 3 μM KU-60019 completely inhibits p53 phosphorylation and partial inhibits at 1 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 display a statistically significant slowing in growth. This growth inhibition is especially evident at the start of the experiment (days 5-12) just after KU-60019 is administered (days 1-5)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 925701-46-8
Appearance Solid
Molecular Weight 547.67
Formel C₃₀H₃₃N₃O₅S
Color Light yellow to khaki
SMILES

C[C@@H]1O[C@@H](CN(CC(NC2=CC3=C(C=C2)SC4=C(C3)C=CC=C4C5=CC(C=C(O5)N6CCOCC6)=O)=O)C1)C
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (28)

All Cell Proliferation/Viability AssayWBCell Imaging/Staining

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Journal Impact Factor

Cell Stem Cell

Minimizing far-extending chromatin perturbation in genome editing preserves stem cell identity. [Abstract]

2026 Mar 5;33(3):470-486.e14. PMID: 41742419
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Acta Biomater

Ataxia telangiectasia mutated inhibitor-loaded copper sulfide nanoparticles for low-temperature photothermal therapy of hepatocellular carcinoma. [Abstract]

2021 Jun:127:276-286. PMID: 33812073
Acta Pharmacol Sin

Targeting DNA-PK overcomes acquired resistance to third-generation EGFR-TKI osimertinib in non-small-cell lung cancer. [Abstract]

2021 Apr;42(4):648-654. PMID: 33414509
Neoplasia

Combined Inhibition of ATR and WEE1 as a Novel Therapeutic Strategy in Triple-Negative Breast Cancer. [Abstract]

2018 Mar 28;20(5):478-488. PMID: 29605721

KU-60019 purchased from MedChemExpress. Usage Cited in: Neoplasia. 2018 Mar 28;20(5):478-488. [Abstract]

MDA-MB-231 and Hs578t cells were treated with 0.05–50 µM of AZD1775 in combination with 0.1–10 µM of ATRi, ATMi (KU-60019) or DNA-PKi for 72 h. Cell viability was detected by CCK-8 assay (n = 3, means).
Cell Rep

FBXW7 Confers Radiation Survival by Targeting p53 for Degradation. [Abstract]

2020 Jan 14;30(2):497-509.e4. PMID: 31940492
Oncogenesis

SCFβ-TrCP-mediated degradation of TOP2β promotes cancer cell survival in response to chemotherapeutic drugs targeting topoisomerase II. [Abstract]

2020 Feb 3;9(2):8. PMID: 32015321

KU-60019 purchased from MedChemExpress. Usage Cited in: Oncogenesis. 2020 Feb 3;9(2):8. [Abstract]

KU60019 (5 μM, 3 h) abolished VM-26-induced TOP2β degradation in SK-BR3 and MDA-MB-231 cells.

KU-60019 purchased from MedChemExpress. Usage Cited in: Oncogenesis. 2020 Feb 3;9(2):8. [Abstract]

The half-life of TOP2β protein was significantly extended in the presence of KU60019 (5 μM, 1 h).
EMBO Rep

Tumor acidosis-induced DNA damage response and tetraploidy enhance sensitivity to ATM and ATR inhibitors. [Abstract]

2024 Mar;25(3):1469-1489. PMID: 38366255

KU-60019 purchased from MedChemExpress. Usage Cited in: EMBO Rep. 2024 Mar;25(3):1469-1489. [Abstract]

Cell viability assays were performed in HCT116 and HT-29 cancer cells cultured at pH 7.4 or 6.5 and treated with the indicated doses of ATMi KU60019 for 72 h.
Breast Cancer Res

NOTCH1 inhibition enhances immunogenicity and sensitizes triple-negative breast cancer to immune checkpoint inhibitors. [Abstract]

2025 May 26;27(1):92. PMID: 40420289

KU-60019 purchased from MedChemExpress. Usage Cited in: Breast Cancer Res. 2025 May 26;27(1):92. [Abstract]

Senescence was detected by SA-β-Gal staining after MDA-MB-231 cells were treated with shNOTCH1 plasmid or KU60019 (3 μM, 48 h).
Int J Mol Sci

Loss of Brcc3 in Zebrafish Embryos Increases Their Susceptibility to DNA Damage Stress. [Abstract]

2024 Nov 11;25(22):12108. PMID: 39596176
Int J Mol Sci

The Effects and Mechanism of ATM Kinase Inhibitors in Toxoplasma gondii. [Abstract]

2024 Jun 25;25(13):6947. PMID: 39000057
Cancers (Basel)

In Vitro and In Silico Investigation of BCI Anticancer Properties and Its Potential for Chemotherapy-Combined Treatments. [Abstract]

2023 Sep 6;15(18):4442. PMID: 37760412
FASEB J

Downregulation of miR-1270 mediates endothelial progenitor cell function in preeclampsia: Role for ATM in the Src/VE-cadherin axis. [Abstract]

2022 Jul;36(7):e22379. PMID: 35648632
J Mol Med (Berl)

Combination of PARP inhibitor and temozolomide to suppress chordoma progression. [Abstract]

2019 Aug;97(8):1183-1193. PMID: 31201471
iScience

Nucleolar stress facilitates islet β cell senescence via hijacking the DNA damage response pathways. [Abstract]

2025 Sep 4;28(10):113508. PMID: 41031371
iScience

BxPC-3-Derived Small Extracellular Vesicles Induce FOXP3+ Treg through ATM-AMPK-Sirtuins-Mediated FOXOs Nuclear Translocations. [Abstract]

2020 Aug 21;23(8):101431. PMID: 32798974
Sci Rep

ATM inhibitor KU60019 synergistically sensitizes lung cancer cells to topoisomerase II poisons by multiple mechanisms. [Abstract]

2023 Jan 17;13(1):882. PMID: 36650267
Cell Signal

MYC amplification sensitizes TNBC to CHK1 inhibitors. [Abstract]

2025 Jul:131:111709. PMID: 40037423
Am J Pathol

Low-Dose Radiotherapy Attenuates Pulmonary Granulomas Involving Ataxia-Telangiectasia Mutated-Dependent Modulation of the Interferon-β Response: A Host-Directed Therapeutic Strategy for Tuberculosis. [Abstract]

2026 Jun 10:S0002-9440(26)00163-X. PMID: 42270072
World J Stem Cells

Hypoxia facilitates triple-negative breast cancer stem cells enrichment and stemness maintenance through oxidized ataxia telangiectasia mutated-induced one-carbon metabolism. [Abstract]

2026 Jan 26;18(1):112278. PMID: 41608656
University of North Carolina at Chapel Hill

2026.
University of Califomia San Francisco

2026.
Res Sq

Small Molecule Activators of the Mitochondrial Protease ClpP Induce Senescence in Triple-Negative Breast Cancer Cells and Sensitize Cells to the Bcl-2 Inhibitor Venetoclax. [Abstract]

2025 Nov 19:rs.3.rs-7682325. PMID: 41333384
bioRxiv

2025 Aug 21.
Authorea

2025 Aug 22.
University of Gothenburg

2023 Jun 27.
Technische Universitat Darmstadt

2022 Aug.
Oxid Med Cell Longev

Inhibition of PLK3 Attenuates Tubular Epithelial Cell Apoptosis after Renal Ischemia-Reperfusion Injury by Blocking the ATM/P53-Mediated DNA Damage Response. [Abstract]

2022 Jun 24;2022:4201287. PMID: 35783188

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (182.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 10 mg/mL (18.26 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8259 mL

9.1296 mL

18.2592 mL

5 mM

0.3652 mL

1.8259 mL

3.6518 mL

10 mM

0.1826 mL

0.9130 mL

1.8259 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Cell Assay^[1]

Cell growth is determined by AlamarBlue. U1242 cells are 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 is added to the medium to the recommended final concentration. Plates are 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[2]

Mice^[2]
Cells (3×10⁷) are implanted into male Fox Chase Severe Combined Immunodeficiency (SCID) mice. Administration of Doxycycline is started when tumors reach 100 mm³ in volume and is performed every 48 hours up to removal of the animal from the experiment. Forty-eight hours after PTEN induction, animals are administered KU-60019 (100 mg/kg) for 5 consecutive days and measured until they reach a target 400 mm³ volume. Measurements of tumor volume and body weight took place every 3 days using calipers.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

[2]. 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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	1.8259 mL	9.1296 mL	18.2592 mL	45.6479 mL
	5 mM	0.3652 mL	1.8259 mL	3.6518 mL	9.1296 mL
	10 mM	0.1826 mL	0.9130 mL	1.8259 mL	4.5648 mL
	15 mM	0.1217 mL	0.6086 mL	1.2173 mL	3.0432 mL
DMSO	20 mM	0.0913 mL	0.4565 mL	0.9130 mL	2.2824 mL
	25 mM	0.0730 mL	0.3652 mL	0.7304 mL	1.8259 mL
	30 mM	0.0609 mL	0.3043 mL	0.6086 mL	1.5216 mL
	40 mM	0.0456 mL	0.2282 mL	0.4565 mL	1.1412 mL
	50 mM	0.0365 mL	0.1826 mL	0.3652 mL	0.9130 mL
	60 mM	0.0304 mL	0.1522 mL	0.3043 mL	0.7608 mL
	80 mM	0.0228 mL	0.1141 mL	0.2282 mL	0.5706 mL
	100 mM	0.0183 mL	0.0913 mL	0.1826 mL	0.4565 mL

Keywords

KU-60019

28 Cited Publications

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KU-60019

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Glucose Metabolism Compound Library

Cancer Stem Cells Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Publications Citing Use of MedChemExpress (MCE) KU-60019

Alle ATM/ATR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (28)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

KU-60019

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Glucose Metabolism Compound Library

Cancer Stem Cells Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Publications Citing Use of MedChemExpress (MCE) KU-60019

Alle ATM/ATR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (28)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

KU-60019 Related Classifications

HY-12061 Related Classifications