| 货号 | 14873-100ug |
| 描述 | Damaged DNA in humans is detected by sensor proteins that transmit a signal through checkpoint kinases (Chks) Chk1 and Chk2.1 Debromohymenialdisine (DBH) is a marine sponge alkaloid that inhibits Chk1 and Chk2 (IC50 = 3 and 3.5 µM, respectively), blocking G2arrest.2,3 Because it does not significantly affect the activity of ataxia-telangiectasia mutated (ATM) or ATM-Tad2-related protein, DBH is a useful tool for studying the roles of Chk1 and Chk2 in DNA repair and cell cycle regulation.2 DBH also inhibits MAP kinase kinase 1 (IC50 = 881 nM), glycogen synthase kinase 3β (IC50 = 1.39 μM), cyclin-dependent kinase 5/p25 (IC50 = 9.12 μM), protein tyrosine kinase 6 (IC50 = 0.6 μM), and other kinases largely unrelated to DNA damage/repair and cell cycling.4,5,6,7 |
| 别名 | DBH;SKF 108753; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Kawabe, T. G2 checkpoint abrogators as anticancer drugs. Molecular Cancer Therapeutics 3(4), 513-519 (2004). 2.Curman, D.,Cinel, B.,Williams, D.E., et al. Inhibition of the G2 DNA damage checkpoint and of protein kinases Chk1 and Chk2 by the marine sponge alkaloid debromohymenialdisine. The Journal of Biological Chemisty 276(21), 17914-17919 (2001). 3.Saleem, R.S.Z.,Lansdell, T.A. and Tepe, J.J. Synthesis and evaluation of debromohymenialdisine-derived Chk2 inhibitors. Bioorganic & Medicinal Chemistry 20(4), 1475-1481 (2012). 4.Tasdemir, D.,Mallon, R.,Greenstein, M., et al. Aldisine alkaloids from the Philippine sponge Stylissa massa are potent inhibitors of mitogen-activated protein kinase kinase-1 (MEK-1). Journal of Medicinal Chemistry 45(2), 529-532 (2002). 5.Wan, Y.,Hur, W.,Cho, C.Y., et al. Synthesis and target identification of hymenialdisine analogs. Chemistry & Biology 11(2), 247-259 (2004). 6.Jobson, A.G.,Cardellina, J.H., II,Scudiero, D., et al. Identification of a bis-guanylhydrazone [4,4-diacetyldiphenylurea-bis(guanylhydrazone); NSC 109555] as a novel chemotype for inhibition of Chk2 kinase. Molecular Pharmacology 72(4), 876-884 (2007). 7.Foloppe, N.,Fisher, L.M.,Francis, G., et al. Identification of a buried pocket for potent and selective inhibition of Chk1: Prediction and verification. Bioorganic & Medicinal Chemistry 14(6), 1792-1804 (2006). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 245.2 |
| 分子式 | C11H11N5O2 |
| CAS号 | 75593-17-8 |
| 稳定性 | ≥ 2 years |
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