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Réactifs et instruments pour l'immunologie, la biologie cellulaire et la biologie moléculaire.

KU-57788 [503468-95-9]

Imprimer

Référence HY-11006-50mg

Conditionnement : 50mg

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Description

KU-57788 (NU7441) is a highly potent and selective DNA-PK inhibitor with an IC₅₀ of 14 nM. KU-57788 is an NHEJ pathway inhibitor. KU-57788 also inhibits PI3K and mTOR with IC₅₀s of 5.0 and 1.7 μM, respectively^[1].

IC₅₀ & Target^[1]

DNA-PK

14 nM (IC₅₀)

mTOR

1.7 μM (IC₅₀)

PI3K

5.0 μM (IC₅₀)

CRISPR/Cas9

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	14 μM Compound: 2, NU7441	Inhibition of human ERG expressed in cisapride treated CHO cells by Ion Works assay Inhibition of human ERG expressed in cisapride treated CHO cells by Ion Works assay	[PMID: 23855836]
Cortical neurone	EC₅₀	1.2 μM Compound: NU7441	Neuroprotective activity in rat cortical neurons transfected with an mHTT-exon1-Q73 construct in presence of primary corticostriatal co-culture system assessed as rescue from mHTT-induced survival loss by fluorescent reporter based assay Neuroprotective activity in rat cortical neurons transfected with an mHTT-exon1-Q73 construct in presence of primary corticostriatal co-culture system assessed as rescue from mHTT-induced survival loss by fluorescent reporter based assay	[PMID: 30840447]
HeLa	EC₅₀	212 nM Compound: 2, NU7441	Inhibition of DNA-PK autophosphorylation at S2056 in human HeLa cells Inhibition of DNA-PK autophosphorylation at S2056 in human HeLa cells	[PMID: 23855836]
HeLa	IC₅₀	14 nM Compound: Chemical Probe: NU7441	Inhibition of human HeLa cell nuclear extract purified DNA-PK using p53 peptide as substrate by ELISA Inhibition of human HeLa cell nuclear extract purified DNA-PK using p53 peptide as substrate by ELISA	[PMID: 16707462]
LoVo	GI₅₀	0.52 μM Compound: Chemical Probe: NU7441	Growth inhibition of human LoVo cells measured after 5 days by crystal violet staining based assay Growth inhibition of human LoVo cells measured after 5 days by crystal violet staining based assay	[PMID: 16707462]

In Vitro

NU7441 (0.5 to 10 μM) inhibits the growth of liver cancer HepG2 cells dose- and time-dependently. NU7441 reduces pDNA-PKcs (S2056) protein expression in liver cancer cells. Furthermore, double treatment of NU7441 and 60Coγ IR affects DNA damage repair^[2].
NU7441 is solvent-exposed in BRD4, this inhibitor can be classified as a Type I BRD inhibitor^[4].
NU7441 reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage^[5].

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

Solvant et solubilité

In Vitro:

DMSO : 6.67 mg/mL (16.13 mM; ultrasonic and warming and heat to 60°C; 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	2.4184 mL	12.0922 mL	24.1844 mL
5 mM	0.4837 mL	2.4184 mL	4.8369 mL
10 mM	0.2418 mL	1.2092 mL	2.4184 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: ≥ 0.67 mg/mL (1.62 mM); Clear solution

This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 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: ≥ 0.67 mg/mL (1.62 mM); Clear solution

This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 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: ≥ 0.67 mg/mL (1.62 mM); Clear solution

This protocol yields a clear solution of ≥ 0.67 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 (6.7 mg/mL) to 900 μL Corn oil, and mix evenly.

Pureté et documentation

Purity: 99.95%

Fiche technique (290 KB) SDS (396 KB)

COA (268 KB) HNMR (274 KB) RP-HPLC (243 KB) LCMS (93 KB) Elemental Analysis Report (127 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Justin J J Leahy, et al. Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries. Bioorg Med Chem Lett. 2004 Dec 20;14(24):6083-7. [Content Brief]

[2]. Yang C, et al. NU7441 Enhances the Radiosensitivity of Liver Cancer Cells. Cell Physiol Biochem. 2016;38(5):1897-905 [Content Brief]

[3]. Hardcastle IR, et al. Discovery of potent chromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK) using a small-molecule library approach. J Med Chem. 2005 Dec 1;48(24):7829-46 [Content Brief]

[4]. Ember SW, et al. The acetyl-lysine binding site of bromodomain-containing protein 4 (BRD4) interacts with diverse kinase inhibitors. ACS Chem Biol. 2014 Feb 25. [Content Brief]

[5]. Robert F, et al. Pharmacological inhibition of DNA-PK stimulates Cas9-mediated genome editing. Genome Med. 2015 Aug 27;7:93 [Content Brief]

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Référence HY-11006-50mg

Contactez votre distributeur local :

Marque : MedChemExpress

Contactez votre distributeur local :

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