SB 218078

Catalog # Availability Size / Price Qty
2560/1
2560/10
SB 218078 | CAS No. 135897-06-2 | Checkpoint Kinase Inhibitors
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Description: Chk1 inhibitor

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%

Product Details
Citations (6)
Reviews

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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

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Citations for SB 218078

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6 Citations: Showing 1 - 6

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