[CAS NO. 503468-95-9] KU-57788
PRODUCTS SPECIFICATIONS [503468-95-9]
DESCRIPTION [503468-95-9]
Overview
| MDL | MFCD11983069 |
|---|---|
| Molecular Weight | 413.49 |
| Molecular Formula | C25H19NO3S |
| SMILES | O=C1C=C(N2CCOCC2)OC3=C1C=CC=C3C4=CC=CC5=C4SC6=C5C=CC=C6 |
17 Publications Citing Use of MCE
- [1]Cell Metab. 2021 Jul 28;S1550-4131(21)00325-9.
- [2]Genome Res. 2021 Mar;31(3):461-471.
- [3]Genome Biol. 2021 Aug 20;22(1):236.
- [4]J Cell Biol. 2022 Nov 7;221(11):e202202100.
- [5]J Cell Biol. 2021 Feb 1;220(2):e201911025.
- [6]PLoS Biol. 2021 Mar 31;19(3):e3001176.
- [7]J Exp Clin Cancer Res. 2022 Apr 12;41(1):140.
- [8]Cell Death Dis. 2020 Jul 30;11(7):602.
- [9]Neoplasia. 2018 Mar 28;20(5):478-488.
- [10]J Cereb Blood Flow Metab. 2022 Dec 19;271678X221147056.
- [11]Int J Mol Sci. 2022, 23(14), 7518.
- [12]J Mol Med (Berl). 2019 Aug;97(8):1183-1193.
- [13]Molecules. 2020 Apr 23;25(8):1980.
- [14]Radiat Res. 2021 May 1;195(5):412-426.
- [15]Mutat Res-Gen Tox En. 2021 Jul;867:503372.
- [16]University of Duisburg-Essen. 2020 Jul.
- [17]Harvard Medical School LINCS LIBRARY
Summary
IC50 & Target
|
DNA-PK 14 nM (IC 50 ) |
mTOR 1.7 μM (IC 50 ) |
PI3K 5.0 μM (IC 50 ) |
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 IC 50 s 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.
Appearance
Solid
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
DMSO : 14.29 mg/mL ( 34.56 mM ; Need ultrasonic)
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 |
-
1.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 1.43 mg/mL (3.46 mM); Clear solution
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.
- [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