KU-57788
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].
Product Specifications
CAS Number
503468-95-9
Product Name Alternative
NU7441
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
CRISPR/Cas9; DNA-PK
Type
Reference compound
Related Pathways
Cell Cycle/DNA Damage; PI3K/Akt/mTOR
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/KU-57788.html
Purity
99.95
Solubility
DMSO : 6.67 mg/mL (ultrasonic; warming; heat to 60°C)
Smiles
O=C1C=C(N2CCOCC2)OC3=C1C=CC=C3C4=CC=CC5=C4SC6=C5C=CC=C6
Molecular Formula
C25H19NO3S
Molecular Weight
413.49
Precautions
H302, H315, H319, H335
References & Citations
[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.|[2]Yang C, et al. NU7441 Enhances the Radiosensitivity of Liver Cancer Cells. Cell Physiol Biochem. 2016;38 (5) :1897-905|[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|[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.|[5]Robert F, et al. Pharmacological inhibition of DNA-PK stimulates Cas9-mediated genome editing. Genome Med. 2015 Aug 27;7:93
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
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