Reagenti e strumenti per immunologia, biologia cellulare e biologia molecolare

KU-55933 [587871-26-9]

Stampa

Cat# HY-12016-10mg

Size : 10mg

Marca : MedChemExpress

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Description

KU-55933 is a potent ATM inhibitor with an IC₅₀ and K_i of 12.9 and 2.2 nM, respectively, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR.

IC₅₀ & Target^[1]

ATM

12.9 nM (IC₅₀)

DNA-PK

2500 nM (IC₅₀)

mTOR

9300 nM (IC₅₀)

PI3K

16600 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC₅₀	1.8 μM Compound: 151C	Inhibition of DNA-PK in HeLa cell nuclear extracts Inhibition of DNA-PK in HeLa cell nuclear extracts	[PMID: 17371003]
HeLa	IC₅₀	14 nM Compound: 42, KU-0055933	Inhibition of ATM isolated from human HeLa cell extract using glutathione S-transferase-p53N66 as substrate by ELISA Inhibition of ATM isolated from human HeLa cell extract using glutathione S-transferase-p53N66 as substrate by ELISA	[PMID: 22835870]
HT-29	IC₅₀	>30 μM Compound: 1; KU-55933	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]
HT-29	IC₅₀	1.22 μM Compound: 1; KU-55933	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]
MCF7	IC₅₀	0.3 μM Compound: 1; KU55933	Inhibition of ATM kinase in human MCF7 cells after 1 hr by immunofluorescence assay Inhibition of ATM kinase in human MCF7 cells after 1 hr by immunofluorescence assay	[PMID: 26632965]
MCF7	IC₅₀	24.8 μM Compound: 1; KU-55933	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]
SW480	IC₅₀	26.5 μM Compound: 1; KU-55933	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]
U2OS	IC₅₀	250 nM Compound: 1; KU55933	Inhibition of ATM in human U2OS cells assessed as inhibition of p53 phosphorylation at Ser15 residue Inhibition of ATM in human U2OS cells assessed as inhibition of p53 phosphorylation at Ser15 residue	[PMID: 26632965]

In Vitro

KU-55933 (10 μM) blocks the ionizing radiation-induced p53 serine 15 phosphorylation. KU-55933 has a dose-dependent effect in inhibiting this ATM-dependent phosphorylation event with an estimated IC₅₀ of 300 nM. KU-55933 ablates the ionizing radiation-induced phosphorylation of these ATM substrates. KU-55933 specifically inhibits ATM but not the other DNA damage-activated PIKKs, ATR, and DNA-PK^[1]. KU-55933 induces pATM, p53, E2F1 and pATR, noticeably upregulates the nuclear fraction of E2F1 at the 0.5 h time point^[2].

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

Solvant et solubilité

In Vitro:

DMSO : 50 mg/mL (126.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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	5.0570 mL
10 mM	0.2529 mL	1.2643 mL	2.5285 mL

View the Complete Stock Solution Preparation Table

* 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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

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 (6.32 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.32 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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Pureté et documentation

Purity: 99.92%

Fiche technique (284 KB) SDS (393 KB)

COA (254 KB) LCMS (93 KB) Elemental Analysis Report (113 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Hickson I, et al. Identification and characterization of a novel and specific inhibitor of the ataxia-telangiectasia mutated kinase ATM. Cancer Res. 2004 Dec 15;64(24):9152-9 [Content Brief]

[2]. Khalil HS, et al. Pharmacological inhibition of ATM by KU55933 stimulates ATM transcription.Exp Biol Med (Maywood). 2012 Jun;237(6):622-34. Epub 2012 Jun 22. [Content Brief]

[3]. Kim YD, et al. Orphan nuclear receptor SHP negatively regulates growth hormone-mediated induction of hepatic gluconeogenesis through inhibition of STAT5 transactivation.J Biol Chem. 2012 Sep 12. [Content Brief]

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HY-12016-5mg

KU-55933 [587871-26-9]

5mg

KU-55933 [587871-26-9]

Cat# HY-12016-10mg

Marca : MedChemExpress

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