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KU-57788

Catalog No. T6276 CAS 503468-95-9

Synonyms: NU7441

NU7441 (KU-57788 (NU7441)) is a highly effective and specific DNA-PK inhibitor (IC50: 14 nM).

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KU-57788, CAS 503468-95-9

Pack Size	Availability	Price/USD
2 mg	In stock	$ 34.00
5 mg	In stock	$ 54.00
10 mg	In stock	$ 90.00
25 mg	In stock	$ 175.00
50 mg	In stock	$ 297.00
100 mg	In stock	$ 413.00
500 mg	In stock	$ 979.00
1 mL * 10 mM (in DMSO)	In stock	$ 64.00

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Purity: 100%

Purity: 99.87%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	NU7441 (KU-57788 (NU7441)) is a highly effective and specific DNA-PK inhibitor (IC50: 14 nM).
Targets&IC50	DNA-PK:13 nM (cell free)
In vitro	0.3 μM of KU-57788 (NU7441), nontoxic to both normal and tumor cells, caused a significant radio-sensitization in tumor cells exposed to X-rays and carbon ions. This concentration did not seem to cause inhibition of DNA DSB repair but induced a significant G2/M arrest [1]. The addition of NU7441 to cells following introduction of the Cas9/sgGFP editing system and the ΔGFP repair template caused a decrease of approximately 40 % in NHEJ events which was accompanied by an approximately two-fold stimulation in HDR. This effect was dose-dependent and reached a maximum at approximately 2.0 μM for NU7441 [2]. NU7441 reduced the CCK-8 counts in the HepG2 culture, further enhanced 60Cox03B3; radiation injury to HepG2 cells, which was manifested by decreasing the DNA-PKcs (S2056) protein expression, increasing x03B3 [3]. Even though RPA p34 is still localized into foci following UV-irradiation and inhibitor treatment, treatment of cells with NU7441 eliminates staining for hyperphosphorylated RPA p34 [4].
In vivo	Tumors in control mice reached four times their starting volume (RTV4) at a median time of 5.6 days. Treatment with etoposide phosphate alone caused a tumor growth delay of 2.7 days, which was extended to 5.4 days by coadministration of NU7441 [5].
Cell Research	Cells were irradiated with 290 MeV/n carbon ions (LET: 50 keV/μm) at the Heavy Ion Medical Accelerator in Chiba. The dose rate for carbon ions was 1 Gy/min. X‐ray irradiation was performed using a TITAN‐320 (200 kV, 20 mA) at a dose rate of 1 Gy/min. NU7441 was dissolved in DMSO and stored at ?20°C in a freezer. Cells were pretreated with NU7441 1 h before irradiation, and the drug was kept throughout the experiment [1].
Animal Research	All in vivo experiments were reviewed and approved by the relevant institutional animal welfare committees and done according to national law. We determined the plasma pharmacokinetics after administering NU7441 i.v. at 5 mg/kg in 10% DMSO/10% cyclodextrin in saline or i.p. or orally at 10 mg/kg (dissolved at 1 mg/mL in 40% PEG400/saline) to female BALB/c mice. These were the maximum administrable doses by the route used due to the limit of solubility of NU7441. Mice were killed at intervals up to 360 minutes after NU7441 administration; blood was taken and immediately centrifuged, and the plasma fraction was removed and stored at ?20°C [5].

Synonyms	NU7441
Molecular Weight	413.49
Formula	C25H19NO3S
CAS No.	503468-95-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 14.29 mg/mL (34.56 mM), Sonification is recommended.

References and Literature

1. Sunada S, et al. Nontoxic concentration of DNA-PK inhibitor NU7441 radio-sensitizes lung tumor cells with little effect on double strand break repair. Cancer Sci. 2016 Sep;107(9):1250-5. 2. Robert F, et al. Pharmacological inhibition of DNA-PK stimulates Cas9-mediated genome editing. Genome Med. 2015 Aug 27;7:93. 3. Yang C, et al. NU7441 Enhances the Radiosensitivity of Liver Cancer Cells. Cell Physiol Biochem. 2016;38(5):1897-905. 4. Cruet-Hennequart S, et al. UV-induced RPA phosphorylation is increased in the absence of DNA polymerase eta and requires DNA-PK. DNA Repair (Amst). 2006 Apr 8;5(4):491-504. 5. Zhao Y, et al. Preclinical evaluation of a potent novel DNA-dependent protein kinase inhibitor NU7441. Cancer Res. 2006 May 15;66(10):5354-62. 6. Zhang B, Wu H, Hao J, et al. Inhibition of DNA-PKcs activity re-sensitizes uveal melanoma cells to radio-and chemotherapy[J]. Biochemical and Biophysical Research Communications. 2019

Citations

1. Zhang B, Wu H, Hao J, et al. Inhibition of DNA-PKcs activity re-sensitizes uveal melanoma cells to radio-and chemotherapy. Biochemical and Biophysical Research Communications. 2019 2. Feng Y L, Liu S C, Chen R D, et al.Proximal binding of dCas9 at a DNA double strand break stimulates homology-directed repair as a local inhibitor of classical non-homologous end joining.Nucleic Acids Research.2023: gkad116.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Antioxidant Compound Library Bioactive Compound Library Target-Focused Phenotypic Screening Library Neuronal Differentiation Compound Library Anti-Liver Cancer Compound Library Neural Regeneration Compound Library Antidepressant Compound Library Oxidation-Reduction Compound Library Anti-Cancer Compound Library

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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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

KU-57788 503468-95-9 DNA Damage/DNA Repair PI3K/Akt/mTOR signaling DNA-PK CRISPR/Cas9 inhibit DNA-dependent protein kinase NU-7441 Inhibitor NU 7441 NU7441 KU 57788 KU57788 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.