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KU 55933

Catalog No.GC11118

An ATM kinase inhibitor

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KU 55933 Chemical Structure

Cas No.: 587871-26-9

Size Price Stock Qty
10mM (in 1mL DMSO)
$52.00
In stock
10mg
$43.00
In stock
50mg
$136.00
In stock
100mg
$262.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Description of KU 55933

KU-55933 is a specific inhibitor of ATM kinase with IC50 value of 13 nM [1].

ATM can stimulate Ser473 phosphorylation of Akt and mediate its full activation in response to insulin. As an ATM inhibitor, KU-55933 significantly inhibited the increase of phospho-Akt at Ser473 in MDA-MB-453 and PC-3 cells treated with insulin and IGF-I following serum starvation. In the MTT assay, KU-55933 treatment suppressed cell proliferation by about 50% at concentration of 10 μM in MDA-MB-453 and PC-3 cells. In a panel of cell lines that have varied Akt activities, KU-55933 treatment caused cell proliferation inhibition correlated with the Akt phosphorylation. KU-55933 was also found to induce G1 cell cycle arrest through down-regulating the cyclin D1 level in MDA-MB-453 and PC-3 cells [2].

References:
[1] Hickson I, Zhao Y, Richardson C J, et al. Identification and characterization of a novel and specific inhibitor of the ataxia-telangiectasia mutated kinase ATM. Cancer research, 2004, 64(24): 9152-9159.
[2] Li Y, Yang D Q. The ATM inhibitor KU-55933 suppresses cell proliferation and induces apoptosis by blocking Akt in cancer cells with overactivated Akt. Molecular cancer therapeutics, 2010, 9(1): 113-125.

Protocol of KU 55933

Cell experiment: [1]

Cell lines

MCF-7 cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

10 μM, 72 hours

Applications

The effect of KU-55933 on viable cell number was measured by counting cells able to exclude Trypan blue. Cell number was significantly reduced by KU-55933. Lactate production was significantly increased in cells treated with KU-55933. Glucose consumption was increased with exposure to KU-55933 treated cells. KU-55933 also decreased ATP levels in MCF-7 cells.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Zakikhani M, Bazile M, Hashemi S, et al. Alterations in cellular energy metabolism associated with the antiproliferative effects of the ATM inhibitor KU-55933 and with metformin. PloS one, 2012, 7(11): e49513.

Chemical Properties of KU 55933

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
Solubility ≥ 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.

Complete Stock Solution Preparation Table of KU 55933

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1 mg 5 mg 10 mg
1 mM 2.5285 mL 12.6425 mL 25.2851 mL
5 mM 0.5057 mL 2.5285 mL 5.057 mL
10 mM 0.2529 mL 1.2643 mL 2.5285 mL
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In vivo Formulation Calculator (Clear solution) of KU 55933

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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.

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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