Chemical Name: 9,10,11,12-Tetrahydro- 9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-1,3(2H)-dione
Biological ActivityInhibitor of checkpoint kinase 1 (Chk1) that displays selectivity over other protein kinases (IC50 values are 15, 250 and 1000 nM for Chk1, cdc2 and PKC respectively). Abrogates G2 cell cycle arrest caused by γ-irradiation and topoisomerase I inhibition. Potentiates cytotoxicity of DNA-damaging drugs, enhancing the efficacy of some chemotherapeutics.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
An indolocarbazole inhibitor of human checkpoint kinase (Chk1) abrogates cell cycle arrest caused by DNA damage.
Jackson et al.
Cancer Res., 2000;60:566
G2 checkpoint abrogators as anticancer drugs.
Mol.Cancer Ther., 2004;3:513
Checkpoint kinase 1-mediated phosphorylation of cdc25C and bad proteins are involved in antitumor effects of loratadine-induced G2/M phase cell-cycle arrest and apoptosis.
Chen et al.
Citations for SB 218078
The citations listed below are publications that use Tocris products. Selected citations for SB 218078 include:
6 Citations: Showing 1 - 6
Cellular responses to a prolonged delay in mitosis are determined by a DNA damage response controlled by Bcl-2 family proteins.
Authors: Colin Et al.
PLoS One 2015;5:140156
The heterogenic final cell cycle of chicken retinal Lim1 horizontal cells is not regulated by the DNA damage response pathway.
Authors: Fard Et al.
Cell Cycle 2013;13:408
Host modulators of H1N1 cytopathogenicity.
Authors: Ward Et al.
PLoS One 2012;7:e39284
Parvovirus B19 infection of human primary erythroid progenitor cells triggers ATR-Chk1 signaling, which promotes B19 virus replication.
Authors: Luo Et al.
J Virol 2011;85:8046
Golgi partitioning controls mitotic entry through Aurora-A kinase.
Authors: Persico Et al.
Mol Biol Cell 2010;21:3708
Synthetic lethal RNAi screening identifies sensitizing targets for gemcit. therapy in pancreatic cancer.
Authors: Azorsa Et al.
J Transl Med 2009;7:43
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