SB 218078

Cat. No. 2560

SB 218078 C24H15N3O3 [135897-06-2]

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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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

Chen et al (2006) 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. Mol.Carcinogenesis 45 461.

Kawabe (2004) G2 checkpoint abrogators as anticancer drugs. Mol.Cancer Ther. 3 513. PMID: 15078995.

Jackson et al (2000) An indolocarbazole inhibitor of human checkpoint kinase (Chk1) abrogates cell cycle arrest caused by DNA damage. Cancer Res. 60 566. PMID: 10676638.

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Citations are publications that use Tocris products. Selected citations for SB 218078 include:

Colin et al (2015) Cellular responses to a prolonged delay in mitosis are determined by a DNA damage response controlled by Bcl-2 family proteins. PLoS One 5 140156. PMID: 25761368.

Fard et al (2013) The heterogenic final cell cycle of chicken retinal Lim1 horizontal cells is not regulated by the DNA damage response pathway. Cell Cycle 13 408. PMID: 24247150.

Ward et al (2012) Host modulators of H1N1 cytopathogenicity. PLoS One 7 e39284. PMID: 22876275.

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Keywords: SB 218078, supplier, inhibitors, inhibits, checkpoint, kinase, 1, Chk1, Chk2, Checkpoint, Kinases, Control, SB218078, Tocris Bioscience, Checkpoint Kinase Inhibitor products

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