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Submit ReviewSB 218078
说明： Chk1 inhibitor
化学名： 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
纯度： ≥98% (HPLC)
生物活性 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.
化合物库 for SB 218078
SB 218078 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for SB 218078
| 分子量 | 393.39 |
| 公式 | C24H15N3O3 |
| 储存 | Store at RT |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for SB 218078
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 39.34 | 100 |
制备储备液 for SB 218078
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for SB 218078
参考文献 for SB 218078
参考文献是支持产品生物活性的出版物。
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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关键词: SB 218078, SB 218078 supplier, inhibitors, inhibits, checkpoint, kinase, 1, Chk1, Chk2, Checkpoint, Kinases, Control, SB218078, 2560, Tocris Bioscience
7 篇 SB 218078 的引用文献
引用文献是使用了 Tocris 产品的出版物。 SB 218078 的部分引用包括：
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
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
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SB 218078 的评论
平均评分: 5 (Based on 1 Review.)
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Combinatorial treatments.
By
MARINA KOUTSIOUMPA on 10/13/2022
分析类型： In Vitro
种属： Human
Combinatorial treatments of SB 218078 with chemotherapeutic drugs resulted in enhanced cytotoxicity in pancreatic and glioma cell lines
该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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.