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Submit ReviewSB 218078
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% (HPLC)
Biological Activity for SB 218078
SB 218078 is an 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 for SB 218078
SB 218078 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for SB 218078
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for SB 218078
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 39.34 | 100 |
Preparing Stock Solutions for SB 218078
The following data is based on the product molecular weight 393.39. Batch specific molecular weights may vary from batch to batch due to the degree 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 for SB 218078
References for SB 218078
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
If you know of a relevant reference for SB 218078, please let us know.
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Keywords: SB 218078, SB 218078 supplier, inhibitors, inhibits, checkpoint, kinase, 1, Chk1, Chk2, Checkpoint, Kinases, Control, SB218078, 2560, Tocris Bioscience
7 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
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
Azorsa et al (2009) Synthetic lethal RNAi screening identifies sensitizing targets for gemcit. therapy in pancreatic cancer. J Transl Med 7 43 PMID: 19519883
Lee et al (2021) A screen of kinase inhibitors reveals a potential role of Chk1 in regulating Hydra head regeneration and maintenance. Int. J. Dev. Biol. 65 523 PMID: 34549798
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
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
Do you know of a great paper that uses SB 218078 from Tocris? Please let us know.
Reviews for SB 218078
Average Rating: 5 (Based on 1 Review.)
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Filter by:
Combinatorial treatments.
By
MARINA KOUTSIOUMPA on 10/13/2022
Assay Type: In Vitro
Species: Human
Combinatorial treatments of SB 218078 with chemotherapeutic drugs resulted in enhanced cytotoxicity in pancreatic and glioma cell lines
Literature in this Area
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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. 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.