KU-57788 (Synonyms: NU7441)

Cat. No.: HY-11006 Purity: 99.73%: FAQs
Data Sheet SDS COA Handling Instructions

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.

KU-57788 Chemical Structure

CAS No. : 503468-95-9

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solution
10 mM * 1 mL in DMSO	USD 80	In-stock	Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL ready for reconstitution	USD 80	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 69	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 119	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 360	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 532	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 18 publication(s) in Google Scholar

18 Publications Citing Use of MCE KU-57788

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Biological Activity
Protocol
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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

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].

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

In Vivo

KU-57788 (0.5 to 10 µM) inhibits the growth of liver cancer HepG2 cells dose- and time-dependently. KU-57788 reduces pDNA-PKcs (S2056) protein expression in liver cancer cells. Furthermore, double treatment of KU-57788 and 60Coγ IR affects DNA damage repair^[2]. KU-57788 weakly inhibits BRD4 and BRDT with IC₅₀s of 1 μM and 3.5 μM, respectively. KU-57788 is solvent-exposed in BRD4, this inhibitor can be classified as a Type I BRD inhibitor^[4]. KU-57788 reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage^[5].

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

Molecular Weight

413.49

Appearance

Solid

Formula

C₂₅H₁₉NO₃S

CAS No.

503468-95-9

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	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 14.29 mg/mL (34.56 mM; Need ultrasonic)

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

*Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO 90% corn oil
Solubility: ≥ 1.43 mg/mL (3.46 mM); Clear solution

*All of the co-solvents are available by MCE.

Purity & Documentation

Purity: 99.73%

Select Batch:

Data Sheet (283 KB) SDS (252 KB)

COA (258 KB) HNMR (260 KB) LCMS (266 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]

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.

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Keywords:

KU-57788503468-95-9NU7441KU57788KU 57788NU 7441NU-7441DNA-PKCRISPR/Cas9DNA-dependent protein kinaseInhibitorinhibitorinhibit

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KU-57788 (Synonyms: NU7441)

Customer Review

18 Publications Citing Use of MCE KU-57788

Featured Recommendations

•Related Screening Libraries:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

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Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

Your Recently Viewed Products:

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