KU-57788 (Synonyms: NU7441)

Name: KU-57788
Brand: MedChemExpress
SKU: HY-11006
Rating: 5.0 (42 reviews)

Cat. No.: HY-11006 Purity: 99.95%: Data Sheet
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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.

For research use only. We do not sell to patients.

CAS No. : 503468-95-9

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
250 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 42 publication(s) in Google Scholar

42 Publications Citing Use of MCE KU-57788

Flow Cytometry

Bio/Physico-chemical Assay

Cell Imaging/Staining

In Vivo Imaging

IHC

Cell Proliferation/Viability Assay

: KU-57788 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jun 3:e2400023. [Abstract]; NU7441 (0-2 μM; 24 h). Morphological changes of NHA/HRasV12/TRIM24 cells treated with NU7441 for 24 h at indicated concentrations.

: KU-57788 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jun 3:e2400023. [Abstract]; NU7441 (20 mg/kg; ip). Representative bioluminescent (BLI) images of treated animals on day 10.

: KU-57788 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jun 3:e2400023. [Abstract]; NU7441 (20 mg/kg; ip). Representative images showing H&E and IHC staining of brain cross sections of NHA/HRas^V12/TRIM24‐derived tumors from animals treated with NU7441 or vehicle for 7 days.

: KU-57788 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jun 3:e2400023. [Abstract]; NU7441 (0.01-100 μM; 48 h). Viability of NHA/HRas^V12 cells with or without ectopic expression of TRIM24 at 48 h after treatment with NU7441.

: KU-57788 purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2024 Oct 22:e180278. [Abstract]; The tumor cell line was treated with DMSO or DNA-PKi (2 μM NU7441) for 48 hours, at which point the drug was washed off prior to coculturing with TILs at a 1:1 ratio for 18 hours. Cytotoxicity was determined by annexin V staining with flow cytometric gating on tumor cells (based on light scatter and CD3^–) and viability dye.

: KU-57788 purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2024 Oct 22:e180278. [Abstract]; B16-F10 melanoma cells were treated with 2 μM NU7441 or DMSO control for 72 hours, at which point gradual darkening was observed.

: KU-57788 purchased from MedChemExpress. Usage Cited in: Cell Metab. 2021 Oct 5;33(10):2076-2089.e9. [Abstract]; FHs 74 Int cells with expression of FLAG-TBK1 were pretreated with NU7441 (1 μM), KU55933 (10 μM),or AZD6738 (2μM) for 2h, and then exposed to 10 Gy ionizing radiation. Immunoprecipitation analyses with anti-FLAG M2 agarose beads were performed 30 min after irradiation.

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Biological Activity
Protocol
Purity & Documentation
References
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Description

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.

Molecular Weight

413.49

Formula

C₂₅H₁₉NO₃S

CAS No.

503468-95-9

Appearance

Solid

Color

White to off-white

SMILES

O=C1C=C(N2CCOCC2)OC3=C1C=CC=C3C4=CC=CC5=C4SC6=C5C=CC=C6

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.95%

Select Batch:

Data Sheet (290 KB) SDS (396 KB)

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

Handling Instructions (2659 KB)

References

[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]

Cell Assay
^[2]

HepG2 cells (4000 per well) are cultured in a 96-well plate for 24 h. Once the cells complete the attachment, 0.1 µM, 1 µM, 5 µM, and 10 µM of KU-57788 are added to the culture media. After 12 h of KU-57788 treatment, 10% CCK-8 solution is added into the culture media, and the incubation continued for two h. OD450 values are determined by a spectrometer, and the results are analyzed to measure the cell growth.

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

References

[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.4184 mL	12.0922 mL	24.1844 mL	60.4610 mL
	5 mM	0.4837 mL	2.4184 mL	4.8369 mL	12.0922 mL
	10 mM	0.2418 mL	1.2092 mL	2.4184 mL	6.0461 mL
	15 mM	0.1612 mL	0.8061 mL	1.6123 mL	4.0307 mL

KU-57788 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KU-57788503468-95-9NU7441KU57788KU 57788NU 7441NU-7441DNA-PKDNA-dependent protein kinaseInhibitorinhibitorinhibit

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KU-57788 (Synonyms: NU7441)

Customer Review

KU-57788 Related Antibodies

42 Publications Citing Use of MCE KU-57788

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Biological Activity

Protocol

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References

Customer Review

KU-57788 Related Antibodies

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Complete Stock Solution Preparation Table

KU-57788 Related Classifications

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