SB 218078
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
Purity: ≥98%
Biological Activity
SB 218078 is an inhibitor 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Host modulators of H1N1 cytopathogenicity.
Ward S, Kim H, Komurov K, Mendiratta S, Tsai P, Schmolke M, Satterly N, Manicassamy B, Forst C, Roth M, Garcia-Sastre A, Blazewska K, McKenna C, Fontoura B, White M
PLoS ONE, 2012;7(8):e39284. -
Cisplatin sensitivity mediated by WEE1 and CHK1 is mediated by miR-155 and the miR-15 family.
Pouliot L, Chen Y, Bai J, Guha R, Martin S, Gottesman M, Hall M
Cancer Res, 2012;72(22):5945-55. -
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.
Kawabe
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.
Mol.Carcinogenesis, 2006;45:461
Product Datasheets
Citations for SB 218078
The citations listed below are publications that use Tocris products. Selected citations for SB 218078 include:
7 Citations: Showing 1 - 7
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A screen of kinase inhibitors reveals a potential role of Chk1 in regulating Hydra head regeneration and maintenance.
Authors: Lee Et al.
Int. J. Dev. Biol. 2021;65:523
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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
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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
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Host modulators of H1N1 cytopathogenicity.
Authors: Ward Et al.
PLoS One 2012;7:e39284
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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
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Golgi partitioning controls mitotic entry through Aurora-A kinase.
Authors: Persico Et al.
Mol Biol Cell 2010;21:3708
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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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