Home Tools

Cart

KU-55933

Catalog No. T2685 CAS 587871-26-9

Synonyms: ATM Kinase Inhibitor

KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

KU-55933, CAS 587871-26-9

Pack Size	Availability	Price/USD
5 mg	In stock	$ 43.00
10 mg	In stock	$ 61.00
25 mg	In stock	$ 103.00
50 mg	In stock	$ 166.00
100 mg	In stock	$ 288.00
1 mL * 10 mM (in DMSO)	In stock	$ 48.00

Bulk Inquiry

Select Batch

Purity: 100%

Purity: 99.80%

Purity: 98.27%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor.
Targets&IC50	ATM:12.9 nM
In vitro	The ATM inhibitor KU-55933 more significantly impacts TRAIL-mediated apoptosis compared to the JAK2 inhibitor AG490 or overexpression of STAT3β. KU-55933 suppresses ATM-dependent STAT3 activation, enhancing TRAIL-regulated apoptosis by upregulating DR5 expression. The inhibition of both STAT3 and NF-κB correlates with the downregulation of cFLIP, accompanying an increase in apoptosis levels.
In vivo	KU-55933 is an effective and specific inhibitor of ATM, with an IC50 of 13 nM and a Ki value of 2.2 nM. It inhibits ATM by blocking the activation of downstream TAp63α, thereby enhancing survivability. KU-55933 exhibits dose-dependent inhibition of ATM-dependent phosphorylation with an IC50 of 300 nM. Furthermore, it sensitizes HeLa cells to ionizing radiation and inhibits cancer cell proliferation. KU-55933 also impedes the phosphorylation of Akt induced by growth factors in cancer cells. Additionally, it inhibits DNA-PK and PI3K, with IC50 values of 2.5 and 16.6 μM, respectively, and mTOR activity, with an IC50 of 9.3 μM. At concentrations lower than 30 μM, KU-58050 does not inhibit the ATM-dependent phosphorylation of p53 (at serine 15). Moreover, KU-55933 does not significantly affect UV-induced phosphorylation of H2AX (at serine 139), NBS1 (at serine 343), CHK1 (at serine 345), and SMC1 (at serine 966).
Kinase Assay	Purified enzyme assays: ATM for use in the in vitro assay is obtained from HeLa nuclear extract by immunoprecipitation with rabbit polyclonal antiserum raised to the COOH-terminal 400 amino acids of ATM in buffer containing 25 mM HEPES (pH 7.4), 2 mM MgCl2, 250 mM KCl, 500 μM EDTA, 100 μM Na3VO4, 10% v/v glycerol, and 0.1% v/v Igepal. ATM-antibody complexes are isolated from nuclear extract by incubating with protein A-Sepharose beads for 1 hour and then through centrifugation to recover the beads. In the well of a 96-well plate, ATM-containing Sepharose beads are incubated with 1 μg of substrate glutathione S-transferase–p53N66 (NH2-terminal 66 amino acids of p53 fused to glutathione S-transferase) in ATM assay buffer [25 mM HEPES (pH 7.4), 75 mM NaCl, 3 mM MgCl2, 2 mM MnCl2, 50 μM Na3VO4, 500 μM DTT, and 5% v/v glycerol] at 37 °C in the presence or absence of inhibitor. After 10 minutes with gentle shaking, ATP is added to a final concentration of 50 μM and the reaction continued at 37 °C for an additional 1 hour. The plate is centrifuged at 250 × g for 10 minutes (4 °C) to remove the ATM-containing beads, and the supernatant is removed and transferred to a white opaque 96-well plate and incubated at room temperature for 1.5 hours to allow glutathione S-transferase-p53N66 binding. This plate is then washed with PBS, blotted dry, and analyzed by a standard ELISA technique with a phospho-serine 15 p53 antibody. The detection of phosphorylated glutathione S-transferase-p53N66 substrate is performed in combination with a goat antimouse horseradish peroxidase-conjugated secondary antibody. Enhanced chemiluminescence solution is used to produce a signal and chemiluminescent detection is carried out.
Cell Research	U2OS cells are exposed to ionizing radiation (3, 5, or 15 Gy) or UV (5 or 50 J/m2) and the ATM response determined by Western blot analysis of p53 serine 15 phosphorylation and stabilization of wild-type p53. Whole cell extracts are obtained from each time point, proteins separated by SDS-PAGE, and the ATM-specific increase in phosphorylated serine 15 measured with a p53 phospho-serine 15 specific antibody. Overall p53 stabilization with time is also observed with a p53-specific antibody (DO-1). Similarly, for studying ATM-dependent phosphorylations on H2AX, CHK1, NBS1, and SMC1, the following antibodies are used: CHK1 phospho-serine 345 and NBS1 phospho-serine 343 antibodies. Histone H2A (H-124) and CHK1 antibodies are also used, as well as SMC1 and SMC1 phospho-serine 966 antibodies. For determination of a cellular IC50 for KU-55933, the peak response time for p53 serine 15 phosphorylation of 2 hours is used to monitor inhibition of ATM. KU-55933 is titrated onto cells and preincubated for 1 hour before ionizing radiation. Using scanning densitometry, the percentage inhibition relative to vehicle control is calculated, and the IC50 value is calculated as for the in vitro determinations.(Only for Reference)

Synonyms	ATM Kinase Inhibitor
Molecular Weight	395.49
Formula	C21H17NO3S2
CAS No.	587871-26-9

Storage

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

Solubility Information

Ethanol: 19.8 mg/mL (50 mM)

DMSO: 39.6 mg/mL (100 mM)

References and Literature

1. Hickson I, et al. Cancer Res. 2004, 64(24), 9152-9159. 2. Soleimani R, et al. Aging. 2011, 3(8), 782-793. 3. Ivanov VN, et al. Cancer Res. 2009, 69(8), 3510-3519. 4. Hu L, Li B, Chen G, et al. A novel M phase blocker, DCZ3301 enhances the sensitivity of bortezomib in resistant multiple myeloma through DNA damage and mitotic catastrophe. Journal of Experimental & Clinical Cancer Research. 2020, 39(1): 1-14. 5. Huang C Y, Hsieh F S, Wang C Y, et al. Supplementary Methods Palbociclib enhances radiosensitivity of hepatocellular carcinoma and cholangiocarcinoma via inhibiting ATM-mediated DNA damage response. EUROPEAN JOURNAL OF CANCER.

Citations

1. Huang C Y, Hsieh F S, Wang C Y, et al. Supplementary Methods Palbociclib enhances radiosensitivity of hepatocellular carcinoma and cholangiocarcinoma via inhibiting ATM-mediated DNA damage response. EUROPEAN JOURNAL OF CANCER. 2019 2. Hu L, Li B, Chen G, et al A novel M phase blocker, DCZ3301 enhances the sensitivity of bortezomib in resistant multiple myeloma through DNA damage and mitotic catastrophe. Journal of Experimental & Clinical Cancer Research. 2020, 39(1): 1-14 3. Bi X, Zhang M, Zhou J, et al.Phosphorylated Hsp27 promotes adriamycin resistance in breast cancer cells through regulating dual phosphorylation of c-Myc.Cellular Signalling.2023: 110913. 4. Yu Z Z, Xu B Q, Wang Y Y, et al.GSK2606414 Sensitizes ABCG2-Overexpressing Multidrug-Resistant Colorectal Cancer Cells to Chemotherapeutic Drugs.Biomedicines.2023, 11(11): 3103. 5. Shen X, Xia Y, Lu H, et al.Synergistic targeting of TrxR1 and ATM/AKT pathway in human colon cancer cells.Biomedicine & Pharmacotherapy.2024, 174: 116507.

Related compound libraries

This product is contained In the following compound libraries：

Highly Selective Inhibitor Library Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library Inhibitor Library Anti-Cancer Active Compound Library Anti-Breast Cancer Compound Library Metabolism Compound Library Anti-Cancer Compound Library Glycometabolism Compound Library Angiogenesis related Compound Library

Related Products

Related compounds with same targets

CGK733 Torin 2 ETP-46464 Wortmannin NU6027 M3541 Elimusertib Ceralasertib

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

KU-55933 587871-26-9 Autophagy DNA Damage/DNA Repair PI3K/Akt/mTOR signaling ATM/ATR DNA-PK PI3K mTOR KU55933 Inhibitor inhibit Ataxia telangiectasia mutated KU 55933 ATM and RAD3 related ATM Kinase Inhibitor inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.