Debromohymenialdisine is an inhibitor of G2 DNA damage checkpoint (IC50 = 8 μM) and check point kinases 1 (Chk1) and 2 (Chk2) (IC50 = 3 μM and IC50 = 3.5 μM, respectively). Differing from many other checkpoint inhibitors, Debromohymenialdisine does not inhibit ataxia-telangiectasia mutated (ATM) or ATM-Rad3-related protein. Debromohymenialdisine also inhibits MAP kinase kinase 1 (MEK-1) (IC50 = 881 nM) but is not as potent as 10Z-hymenialdisine (IC50 = 6 nM).
1. Curman, D., et al. 2001. J. Biol. Chem. 276: 17914-17919. PMID: 11279124 2. Tasdemir, D. , et al. 2002. J. Med. Chem. 45: 529-532. PMID: 11784156 3. Kawabe, T. 2004. Mol. Cancer Ther. 3: 513-519. PMID: 15078995
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Kawabe (PubMed ID 15078995) used decromohymenialdisineKawabe (PubMed ID 15078995) used decromohymenialdisine to inhibit CHK1 and CHK2 in cancer cells. -SCBT Publication Review
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