For research use only. Not for therapeutic Use.
CGK733（Cat No.:I005413）is a selective inhibitor of ATM and ATR kinases, key regulators of the DNA damage response and cell cycle checkpoint pathways. By inhibiting these kinases, CGK733 disrupts the repair of DNA damage, leading to cell cycle arrest and apoptosis in cancer cells. It is widely used in research to explore mechanisms of cellular senescence, DNA repair, and tumor progression. CGK733’s ability to sensitize cancer cells to radiation and chemotherapy makes it a valuable tool in studying potential therapeutic approaches that target DNA damage responses in oncology.
| Catalog Number | I005413 |
| CAS Number | 905973-89-9 |
| Synonyms | 2,2-diphenyl-N-[2,2,2-trichloro-1-[(4-fluoro-3-nitrophenyl)carbamothioylamino]ethyl]acetamide |
| Molecular Formula | C₂₃H₁₈Cl₃FN₄O₃S |
| Purity | ≥95% |
| Target | ATM/ATR |
| Solubility | 10 mM in DMSO |
| Storage | Store at -20C |
| IUPAC Name | 2,2-diphenyl-N-[2,2,2-trichloro-1-[(4-fluoro-3-nitrophenyl)carbamothioylamino]ethyl]acetamide |
| InChI | InChI=1S/C23H18Cl3FN4O3S/c24-23(25,26)21(30-22(35)28-16-11-12-17(27)18(13-16)31(33)34)29-20(32)19(14-7-3-1-4-8-14)15-9-5-2-6-10-15/h1-13,19,21H,(H,29,32)(H2,28,30,35) |
| InChIKey | HLCDNLNLQNYZTK-UHFFFAOYSA-N |
| SMILES | C1=CC=C(C=C1)C(C2=CC=CC=C2)C(=O)NC(C(Cl)(Cl)Cl)NC(=S)NC3=CC(=C(C=C3)F)[N+](=O)[O-] |
| Reference | </br>1:CGK733-induced LC3 II formation is positively associated with the expression of cyclin-dependent kinase inhibitor p21Waf1/Cip1 through modulation of the AMPK and PERK/CHOP signaling pathways. Wang Y, Kuramitsu Y, Baron B, Kitagawa T, Tokuda K, Akada J, Nakamura K.Oncotarget. 2015 Nov 24;6(37):39692-701. doi: 10.18632/oncotarget.5625. PMID: 26486079 Free PMC Article</br>2:PERK/CHOP contributes to the CGK733-induced vesicular calcium sequestration which is accompanied by non-apoptotic cell death. Wang Y, Kuramitsu Y, Baron B, Kitagawa T, Akada J, Tokuda K, Cui D, Nakamura K.Oncotarget. 2015 Sep 22;6(28):25252-65. doi: 10.18632/oncotarget.4487. PMID: 26259235 Free PMC Article</br>3:CGK733 enhances multinucleated cell formation and cytotoxicity induced by taxol in Chk1-deficient HBV-positive hepatocellular carcinoma cells. Wang H, Zuo B, Wang H, Ren L, Yang P, Zeng M, Duan D, Liu C, Li M.Biochem Biophys Res Commun. 2012 May 25;422(1):103-8. doi: 10.1016/j.bbrc.2012.04.115. Epub 2012 Apr 30. PMID: 22564734 </br>4:CGK733 does not inhibit ATM or ATR kinase activity in H460 human lung cancer cells. Choi S, Toledo LI, Fernandez-Capetillo O, Bakkenist CJ.DNA Repair (Amst). 2011 Oct 10;10(10):1000-1; author reply 1002. doi: 10.1016/j.dnarep.2011.07.013. Epub 2011 Aug 23. No abstract available. PMID: 21865098 Free PMC Article</br>5:The ATM and ATR inhibitors CGK733 and caffeine suppress cyclin D1 levels and inhibit cell proliferation. Alao JP, Sunnerhagen P.Radiat Oncol. 2009 Nov 10;4:51. doi: 10.1186/1748-717X-4-51. PMID: 19903334 Free PMC Article |
