Catalog Number: 2560
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 Activity
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
  • M.Wt:
    393.39
  • Formula:
    C24H15N3O3
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at RT
  • CAS No:
    135897-06-2
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. An indolocarbazole inhibitor of human checkpoint kinase (Chk1) abrogates cell cycle arrest caused by DNA damage.
    Jackson et al.
    Cancer Res., 2000;60:566
  2. G2 checkpoint abrogators as anticancer drugs.
    Kawabe
    Mol.Cancer Ther., 2004;3:513
  3. 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
Citations:

The citations listed below are publications that use Tocris products. Selected citations for SB 218078 include:

3 Citations: Showing 1 - 3
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  1. 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
  2. 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
  3. Host modulators of H1N1 cytopathogenicity.
    Authors: Ward Et al.
    PLoS One 2012;7:e39284

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