| 货号 | 10549-1mg |
| 描述 | C646 is an inhibitor of the histone acetyltransferase p300 (IC50 = 1.6 μM).1 It competitively (versus acetyl-CoA) binds p300 (Ki = 400 nM) and does not inhibit several other acetyltransferases.1 The action of C646 appears to be irreversible through covalent modification of the enzyme target.1 It blocks the growth of human melanoma, leukemia, lung, and prostate cancer cells in vitro.1,2,3 C646 has been used to study the role of p300-mediated acetylation in such models as fear extinction memory and the regulation of immediate-early genes.4,5 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Bowers, E.M.,Yan, G.,Mukherjee, C., et al. Virtual ligand screening of the p300/CBP histone acetyltransferase: Identification of a selective small molecule inhibitor. Chemistry & Biology 17(5), 471-482 (2010). 2.Gao, X.n.,Lin, J.,Ning, Q.y., et al. A histone acetyltransferase p300 inhibitor C646 induces cell cycle arrest and apoptosis selectively in AML1-ETO-positive AML cells. PLoS One 8(2), (2013). 3.Santer, F.R.,Höschele, P.P.S.,Oh, S.J., et al. Inhibition of the acetyltransferases p300 and CBP reveals a targetable function for p300 in the survival and invasion pathways of prostate cancer cell lines. Molecular Cancer Therapeutics 10(9), 1644-1655 (2011). 4.Marek, R.,Coelho, C.M.,Sullivan, R.K.P., et al. Paradoxical enhancement of fear extinction memory and synaptic plasticity by inhibition of the histone acetyltransferase p300. Journal of Neuroscience 31(20), 7486-7491 (2011). 5.Crump, N.T.,Hazzalin, C.A.,Bowers, E.M., et al. Dynamic acetylation of all lysine-4 trimethylated histone H3 is evolutionarily conserved and mediated by p300/CBP. Proceedings of the National Academy of Sciences of the United States of America 108(19), 7814-7819 (2011). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% (mixture of isomers) |
| 计算分子量 | 445.4 |
| 分子式 | C24H19N3O6 |
| CAS号 | 328968-36-1 |
| 稳定性 | ≥ 2 years |
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