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Category: EnzymesarrowKinasesarrowCheckpoint and Related Kinases
Cat.No. Product Name
2560 SB 218078
Price and Availability

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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

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:

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M.Wt: 393.39
Formula: C24H15N3O3
Storage: Store at RT
Solubility: Soluble to 100 mM in DMSO
Purity: >98%
CAS No: [135897-06-2]

Resources:

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    • Certificate of Analysis / MSDS:

    Certificate of Analysis: View current batch
    Product/Material Safety Data Sheet: View current batch

    References:

    Jackson et al (2000) An indolocarbazole inhibitor of human checkpoint kinase (Chk1) abrogates cell cycle arrest caused by DNA damage. Cancer Res. 60 566. Kawabe (2004) G2 checkpoint abrogators as anticancer drugs. Mol.Cancer Ther. 3 513. 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.
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    Keywords: SB 218078, Kinases, Inhibitor Of Checkpoint Kinase 1 (Chk1), SB218078, Tocris Bioscience
    Literature in this Area
    Signal Transduction Guide
    Signal Transduction Guide : An informative guide for all scientists working in: Cell cycle & apoptosis, Protein kinases & phosphatases, Ion channels, Calcium & lipid signaling, Cyclic nucleotides & G-proteins, Nitric oxide, & Signaling EnzymesA complete listing of signal transduction products available from Tocris, including descriptions on selected tools and unit sizes.
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