SB 218078

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Cat.No. 2560 - SB 218078 | C24H15N3O3 | CAS No. 135897-06-2
Description: Inhibitor of checkpoint kinase 1 (Chk1)
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% (HPLC)
Datasheet
Citations (6)
Reviews
Literature

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.

Compound Libraries

SB 218078 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 393.39
Formula C24H15N3O3
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 135897-06-2
PubChem ID 3387354
InChI Key OTPNDVKVEAIXTI-UHFFFAOYSA-N
Smiles O=C1NC(=O)C2=C1C1=C3N(C4CCC(O4)N4C5=C(C=CC=C5)C2=C34)C2=CC=CC=C12

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 39.34 100

Preparing Stock Solutions

The following data is based on the product molecular weight 393.39. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.54 mL 12.71 mL 25.42 mL
5 mM 0.51 mL 2.54 mL 5.08 mL
10 mM 0.25 mL 1.27 mL 2.54 mL
50 mM 0.05 mL 0.25 mL 0.51 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the biological activity of the product.

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

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

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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View all Checkpoint Kinase Inhibitors

Keywords: SB 218078, SB 218078 supplier, inhibitors, inhibits, checkpoint, kinase, 1, Chk1, Chk2, Checkpoint, Kinases, Control, SB218078, 2560, Tocris Bioscience

6 Citations for SB 218078

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

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

Persico et al (2010) Golgi partitioning controls mitotic entry through Aurora-A kinase. Mol Biol Cell 21 3708 PMID: 20844084

Azorsa et al (2009) Synthetic lethal RNAi screening identifies sensitizing targets for gemcitabine therapy in pancreatic cancer. J Transl Med 7 43 PMID: 19519883

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

Luo et al (2011) Parvovirus B19 infection of human primary erythroid progenitor cells triggers ATR-Chk1 signaling, which promotes B19 virus replication. J Virol 85 8046 PMID: 21680529


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Literature in this Area

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Kinases Product Listing

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Cell Cycle & DNA Damage Repair

Cell Cycle & DNA Damage Repair Poster

In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.