K252a: a new blocker of the cell-cycle at G1 phase in a human hepatoma cell line.
The administration of 200 nM K252a to HuH7 suppressed the proliferation of the cells almost completely. The uptake of [3H]thymidine was inhibited, and flow cytometry revealed only one peak at 2C on day 3 after treatment with 100 nM K252a. The expression of proto-oncogene c-myc was not reduced. Despite the blockage at G1, both the size of the cells and the amount of cell protein had increased by 4 times by day 3 after treatment with K252a, while the cells secreted albumin and alpha-fetoprotein into the medium as usual. These results show that K252a can increase the cell size of HuH7 without losing its function by blocking the cell cycle at G1 phase.
Nakayama
T
T
First Department of Internal Medicine, Faculty of Medicine, University of Tokyo, Japan.
Hashimoto
Y
Y
Kaneko
Y
Y
Yoshida
M
M
Beppu
T
T
Ohmi
K
K
Yamashita
S
S
Nonomura
Y
Y
Kurokawa
K
K
D002227:Carbazoles / Q000494:pharmacology*; D006528:Carcinoma, Hepatocellular / Q000473:pathology*; D002455:Cell Division / Q000187:drug effects; D004247:DNA / Q000096:biosynthesis; D005434:Flow Cytometry; D016193:G1 Phase / Q000187:drug effects*; D015870:Gene Expression; D016259:Genes, myc; D006801:Humans; D026121:Indole Alkaloids; D008113:Liver Neoplasms / Q000473:pathology*; D000090063:Proto-Oncogene Mas; D014407:Tumor Cells, Cultured
D002227:Carbazoles; D026121:Indole Alkaloids; C000715470:MAS1 protein, human; D000090063:Proto-Oncogene Mas; D004247:DNA; C049985:staurosporine aglycone