| 货号 | 13156-10mg |
| 描述 | The methylation of histones by histone methyltransferases (HMT) is an important mechanism by which gene expression is stably altered during cellular differentiation and embryonic development. Chaetocin is a fungal mycotoxin that inhibits the HMT SU(VAR)3-9 (IC50 = 0.8 μM).1 It inhibits other Lys9-specific HMTs, including G9a (IC50 = 2.5 μM) and DIM5 (IC50 = 3 μM).1 Selectivity for Lys9-HMTs is indicated by higher IC50 values (>90 μM) for Lys20-specific PRSET7, Lys27-specific EZH2, and Lys4-specific SET7/9. Chaetocin potently induces cellular oxidative stress, selectively killing cancer cells and rapidly-proliferating primary cells.2,1 Chaetocin’s effects on oxidative stress are, at least in part, due to its capacity to act as a competitive and selective substrate for thioredoxin reductase-1 (Km = 4.6 μM).3 Chaetocin is useful both in epigenetic studies as an HMT inhibitor and in cancer research.4,5,6 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Greiner, D.,Bonaldi, T.,Eskeland, R., et al. Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9. Nature Chemical Biology 1(3), 143-145 (2005). 2.Isham, C.R.,Tibodeau, J.D.,Jin, W., et al. Chaetocin: A promising new antimyeloma agent with in vitro and in vivo activity mediated via imposition of oxidative stress. Blood 109(6), 2579-2588 (2007). 3.Tibodeau, J.D.,Benson, L.M.,Isham, C.R., et al. The anticancer agent chaetocin is a competitive substrate and inhibitor of thioredoxin reductase. Antioxidants & Redox Signaling 11(5), 1097-1106 (2009). 4.Bissinger, E.M.,Heinke, R.,Sippl, W., et al. Targeting epigenetic modifiers: Inhibitors of histone methyltransferases. Med.Chem.Commun. (2010). 5.Spannhoff, A.,Sippl, W., and Jung, M. Cancer treatment of the future: Inhibitors of histone methyltransferases. International Journal of Biochemistry and Cell Biology 41, 4-11 (2009). 6.Copeland, R.A.,Solomon, M.E., and Richon, V.M. Protein methyltransferases as a target class for drug discovery. Nature Reviews.Drug Discovery 8, 724-732 (2009). | |
| 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 | 696.8 |
| 分子式 | C30H28N6O6S4 |
| CAS号 | 28097-03-2 |
| 稳定性 | ≥ 2 years |
| 本官网所有报价均为常温或者蓝冰运输价格，如有产品需要干冰运输，需另外加收干冰运输费。 |