KU 55933 |
| Katalog-Nr.GC11118 |
KU 55933 is a potent and specific ATM kinase inhibitor that sensitizes human tumor cells to ionizing radiation and chemotherapeutic agents. KU 55933 has an IC50 of 13nM and Ki of 2.2nM in vitro.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 587871-26-9
Sample solution is provided at 25 µL, 10mM.
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KU 55933 is a potent and specific ATM kinase inhibitor that sensitizes human tumor cells to ionizing radiation and chemotherapeutic agents[1]. KU 55933 has an IC50 of 13nM and Ki of 2.2nM in vitro[2].
In vitro, The ATM inhibitor KU 55933 (10μM; 1h) suppresses cell proliferation and induces apoptosis by blocking Akt in cancer cells with overactivated Akt[3]. Inhibition of ATM with KU 55933 (10μM; 24h or 72h) sensitizes endometrial cancer cell lines to Olaparib[4]. KU 55933 (0.01-20μM; 24h) is neuroprotective against the doxorubicin-induced cell damage in UN- and RA-SH-SY5Y cells[5].
In vivo, Administration of KU 55933 (8mg/kg; 12 weeks; i.v.) to apolipoprotein E-deficient mice inhibited Smad1/5 activation in endothelial cells (ECs) in atherosclerosis-susceptible regions, thereby suppressing endothelial cell proliferation and inflammation and attenuating atherosclerotic lesions in these mice[3]. KU 55933 (1mg/kg; 4 weeks; i.p.) treatment inhibits tumor growth and metastasis in mouse mammary tumors in vivo through the inhibition of GLUT1 translocation and vimentin expression[6].
References:
[1] Wei SY, Fu WS, Liu CH, et al. Identification of KU-55933 as an anti-atherosclerosis compound by using a hemodynamic-based high-throughput drug screening platform. Proc Natl Acad Sci U S A. 2024 Jan 30;121(5):e2318718121.
[2] Golding SE, Rosenberg E, Valerie N, 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.
[3] Zhang A, Zhang L, Xie X, et al. Inhibition of ATM with KU-55933 Sensitizes Endometrial Cancer Cell Lines to Olaparib. Onco Targets Ther. 2023 Dec 19;16:1061-1071.
[4] Chwastek J, Jantas D, Lasoń W. The ATM kinase inhibitor KU-55933 provides neuroprotection against hydrogen peroxide-induced cell damage via a γH2AX/p-p53/caspase-3-independent mechanism: Inhibition of calpain and cathepsin D. Int J Biochem Cell Biol. 2017 Jun;87:38-53.
[5] Li Y, Yang DQ. The ATM inhibitor KU-55933 suppresses cell proliferation and induces apoptosis by blocking Akt in cancer cells with overactivated Akt. Mol Cancer Ther. 2010 Jan;9(1):113-25.
[6] Harris BRE, Zhang Y, Tao J, et al. ATM inhibitor KU-55933 induces apoptosis and inhibits motility by blocking GLUT1-mediated glucose uptake in aggressive cancer cells with sustained activation of Akt. FASEB J. 2021 Apr;35(4):e21264.
| Cell experiment [1]: | |
Cell lines | Ishikawa and Hec-108 cells |
Preparation Method | Ishikawa and Hec-108 cells were cultured to 30-50% confluence and then treated with Olaparib (50µM) alone or in combination with KU 55933 (10µM) for 24h. The cells were then harvested, washed with cold PBS and stained with PI and FITC-Annexin V. Apoptosis was detected by CytoFLEX and analyzed by CytExpert software. |
Reaction Conditions | 10μM; 24h |
Applications | Inhibition of ATM with KU 55933 sensitizes endometrial cancer cell lines to Olaparib. |
| Animal experiment [2]: | |
Animal models | Six-week-old male ApoE−/− mice |
Preparation Method | ApoE−/− mice fed a high-fat diet (HFD) were tail-vein injected with KU 55933 (8mg/kg) or vehicle (DMSO in saline) for 12 weeks. After the experiment, biochemical analysis was performed on the mouse plasma, and the mouse aorta and aortic roots were stained with Oil Red O and H&E. |
Dosage form | 8mg/kg; 12 weeks; i.v. |
Applications | Administration of KU 55933 to apolipoprotein E-deficient mice inhibited Smad1/5 activation in endothelial cells (ECs) in atherosclerosis-susceptible regions, thereby suppressing endothelial cell proliferation and inflammation and attenuating atherosclerotic lesions in these mice. |
References: | |
| Cas No. | 587871-26-9 | SDF | |
| Chemical Name | 2-morpholin-4-yl-6-thianthren-1-ylpyran-4-one | ||
| Canonical SMILES | C1COCCN1C2=CC(=O)C=C(O2)C3=C4C(=CC=C3)SC5=CC=CC=C5S4 | ||
| Formula | C21H17NO3S2 | M.Wt | 395.49 |
| Löslichkeit | ≥ 41.7mg/mL in DMSO with gentle warming | Storage | Desiccate at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5285 mL | 12.6425 mL | 25.2851 mL |
| 5 mM | 505.7 μL | 2.5285 mL | 5.057 mL |
| 10 mM | 252.9 μL | 1.2643 mL | 2.5285 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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