| 货号 | 18811-500ug |
| 描述 | CREB-binding protein (CBP) and E1A-associated protein p300 are transcriptional co-activators that modulate DNA replication, DNA repair, cell growth, transformation, and development.1,2 Both CBP and p300 contain bromodomains, which mediate their binding to acetylated lysine residues on histones and other proteins.3 PF-CBP1 is an inhibitor of the CBP and p300 bromodomains (IC50s = 125 and 363 nM, respectively).4 It displays greater than 100-fold selectivity for the bromodomain of CBP over those of BRD4 and a panel of other proteins.4 PF-CBP1 reduces the expression of inflammatory cytokines by LPS-stimulated primary macrophages.4 It also suppresses the expression of RGS4 (regulator of G protein signaling 4) in primary cortical neurons.4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Iyer, N.G.,Özdag, H., and Caldas, C. p300/CBP and cancer. Oncogene 23, 4225-4231 (2004). 2.Kalkhoven, E. CBP and p300: HATs for different occasions. Biochemical Pharmacology 68, 1145-1155 (2004). 3.Zeng, L.,Zhang, Q.,Gerona-Navarro, G., et al. Structural basis of site-specific histone recognition by the bromodomains of human coactivators PCAF and CBP/p300. Structure 16(4), 643-652 (2008). 4.Piatnitski Chekler, E.L.,Pellegrino, J.A.,Lanz, T.A., et al. Transcriptional profiling of a selective CREB binding protein bromodomain inhibitor highlights therapeutic opportunities. Chemistry & Biology 22(12), 1588-1596 (2015). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 488.6 |
| 分子式 | C29H36N4O3 |
| 稳定性 | ≥ 2 years |
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