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Submit ReviewNSC 109555 ditosylate is a selective, reversible, ATP-competitive Chk2 inhibitor (IC50 = 0.2 μM) that displays no effect on a range of other kinases including Chk1 (IC50 > 10 μM). Inhibits histone H1 phosphorylation (IC50 = 0.24 μM) and attenuates mitochondrial ATP synthesis. Exhibits antiproliferative activity in a number of leukemias in vivo.
分子量 | 752.86 |
公式 | C19H24N10O.2C7H8O3S |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 66748-43-4 |
PubChem ID | 12449850 |
InChI Key | DIQGNVANOSOABS-XMDRLFCYSA-N |
Smiles | O=C(NC2=CC=C(/C(C)=N/NC(N)=N)C=C2)NC1=CC=C(/C(C)=N/NC(N)=N)C=C1.CC3=CC=C(S(=O)(O)=O)C=C3.CC4=CC=C(S(=O)(O)=O)C=C4 |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 7.53 | 10 |
以下数据基于产品分子量 752.86。 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 |
---|---|---|---|
0.1 mM | 13.28 mL | 66.41 mL | 132.83 mL |
0.5 mM | 2.66 mL | 13.28 mL | 26.57 mL |
1 mM | 1.33 mL | 6.64 mL | 13.28 mL |
5 mM | 0.27 mL | 1.33 mL | 2.66 mL |
参考文献是支持产品生物活性的出版物。
Byczkowski et al (1981) Actions of bis(guanylhydrazones) on isolated rat liver mitochondria. Biochem.Pharmacol. 30 2851 PMID: 6895596
Byczkowski et al (1982) Potentiation of the antimitochondrial and antiproliferative effects of bis(guanylhydrazones) by phenethylbiguanide. Cancer Res. 42 3592 PMID: 6896674
Jobson et al (2007) Identification of a bis-guanylhydrazone [4,4'-diacetyldiphenylurea-bis(guanylhydrazone); NSC 109555] as a novel chemotype for inhibition of Chk2 kinase. Mol.Pharmacol. 72 876 PMID: 17616632
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关键词: NSC 109555 ditosylate, NSC 109555 ditosylate supplier, Selective, Chk2, inhibitors, inhibits, Checkpoint, Kinases, Control, NSC109555, ditosylate, DDUG, 3034, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 NSC 109555 ditosylate 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
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
Duong et al (2013) Inhibition of checkpoint kinase 2 (CHK2) enhances sensitivity of pancreatic adenocarcinoma cells to gemcit. J Cell Mol Med 17 1261 PMID: 23855452
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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。
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.