CGK 733, 2,2-DIPHENYL-N-(2,2,2-TRICHLORO-1-[3-(4-FLUORO-3-NITROPHENYL)THIOUREIDO]ETHYL)ACETAMIDE;CGK733;A-PHENYL-N-[2,2,2-TRICHLORO-1-[[[(4-FLUORO-3-NITROPHENYL)AMINO]THIOXOMETHYL]AMINO]ETHYL]BENZENEACETAMIDE; 905973-89-9
CGK 733 is a small molecule inhibitor reportedly targeting the kinase activities of ATM and ATR.
IC50 Value:
Target: ATM/ATR
in vitro: Culture of MCF-7 breast cancer cells with 10 μM CGK733 induced a detectable decline of cyclin D1 levels within 2 h of exposure, and this effect was maximal between 4 and 6 h after exposure, CGK733 induced the loss of cyclin D1 expression at concentrations as low as 5 μM and this activity was maximal at 10 to 20 μM The CGK733 induced attenuation of cyclin D1 levels was inhibited by the 26S proteasome inhibitor MG132 but not the GSK3β inhibitor lithium chloride (LiCl) in MCF-7 and T47D cells [1]. CGK733 significantly enhanced taxol-induced cytotoxicity in HBV-positive HepG2.2.15 cells. The mechanism lies in CGK733 triggers the formation of multinucleated cells thus promotes the premature mitotic exit of taxol-induced mitotic-damaged cells through multinucleation and mitotic catastrophe in HBV-positive HepG2.2.15 cells [2].
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