For research use only. Not for therapeutic Use.
KU-0060648 is a dual inhibitor of DNA-PK and PI-3K. KU-0060648 inhibited cellular DNA-PK autophosphorylation with IC(50) values of 0.019 μmol/L (MCF7 cells) and 0.17 μmol/L (SW620 cells), and PI-3K-mediated AKT phosphorylation with IC(50) values of 0.039 μmol/L (MCF7 cells) and more than 10 μmol/L (SW620 cells). KU-0060648 inhibits hepatocellular carcinoma cells through DNA-PKcs-dependent and DNA-PKcs-independent mechanisms.
| Catalog Number | R061446 |
| CAS Number | 881375-00-4 |
| Synonyms | 4-Ethyl-N-[4-[2-(4-morpholinyl)-4-oxo-4H-1-benzopyran-8-yl]-1-dibenzothienyl]-1-piperazineacetamide |
| Molecular Formula | C33H34N4O4S |
| Purity | ≥95% |
| Target | PI3K/Akt/mTOR |
| Solubility | Limited solubility |
| Storage | Store at -20°C |
| IUPAC Name | 2-(4-ethylpiperazin-1-yl)-N-[4-(2-morpholin-4-yl-4-oxochromen-8-yl)dibenzothiophen-1-yl]acetamide |
| InChI | InChI=1S/C33H34N4O4S/c1-2-35-12-14-36(15-13-35)21-29(39)34-26-11-10-23(33-31(26)25-6-3-4-9-28(25)42-33)22-7-5-8-24-27(38)20-30(41-32(22)24)37-16-18-40-19-17-37/h3-11,20H,2,12-19,21H2,1H3,(H,34,39) |
| InChIKey | AATCBLYHOUOCTO-UHFFFAOYSA-N |
| SMILES | CCN1CCN(CC1)CC(=O)NC2=C3C4=CC=CC=C4SC3=C(C=C2)C5=CC=CC6=C5OC(=CC6=O)N7CCOCC7 |
| Reference | </br>1:KU-0060648 inhibits hepatocellular carcinoma cells through DNA-PKcs-dependent and DNA-PKcs-independent mechanisms. Chen MB, Zhou ZT, Yang L, Wei MX, Tang M, Ruan TY, Xu JY, Zhou XZ, Chen G, Lu PH.Oncotarget. 2016 Mar 29;7(13):17047-59. doi: 10.18632/oncotarget.7742. PMID: 26933997 Free PMC Article</br>2:Chemosensitization of cancer cells by KU-0060648, a dual inhibitor of DNA-PK and PI-3K. Munck JM, Batey MA, Zhao Y, Jenkins H, Richardson CJ, Cano C, Tavecchio M, Barbeau J, Bardos J, Cornell L, Griffin RJ, Menear K, Slade A, Thommes P, Martin NM, Newell DR, Smith GC, Curtin NJ.Mol Cancer Ther. 2012 Aug;11(8):1789-98. doi: 10.1158/1535-7163.MCT-11-0535. Epub 2012 May 10. PMID: 22576130 Free PMC Article |
