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PF-CBP1 是一种高选择性的 CREB 结合蛋白 (CREBBP) 溴结构域抑制剂。它抑制 CREBBP (IC50: 125 nM) 和 p300 溴结构域 (IC50: 363 nM)。
PF-CBP1 是一种高选择性的 CREB 结合蛋白 (CREBBP) 溴结构域抑制剂。它抑制 CREBBP (IC50: 125 nM) 和 p300 溴结构域 (IC50: 363 nM)。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 145 | 现货 | |
2 mg | ¥ 198 | 现货 | |
5 mg | ¥ 365 | 现货 | |
10 mg | ¥ 642 | 现货 | |
25 mg | ¥ 1,250 | 现货 | |
50 mg | ¥ 2,270 | 现货 | |
100 mg | ¥ 3,250 | 现货 | |
200 mg | ¥ 4,570 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 365 | 现货 |
产品描述 | PF-CBP1 HCl is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP). It inhibits CREBBP (IC50: 125 nM) and p300 bromodomains (IC50: 363 nM). |
靶点活性 | p300 BD:363 nM, CREBBP:125 nM |
体外活性 | PF-CBP1在原代巨噬细胞中调节关键炎症基因。PF-CBP1在神经元中下调RGS4,一个与帕金森病相关的靶点。在生化实验中,PF-CBP1对BRD4的选择性为139倍,通过ITC,选择性>105倍。PF-CBP1还是一种强效的EP300抑制剂,在巨噬细胞中没有细胞毒性。 |
细胞实验 | Cells are pretreated with the probes PF-CBP1, ISOX-INACT, or ISOX-DUAL starting at 10 μM concentrations, and then serially diluted to 0.1 μM. After 30 min, the cells are treated with LPS to induce gene transcription and the expression levels of interleukin-6 (IL-6), IL-1β, and interferon-β (IFN-β)(which are known to be induced after 4 h of LPS exposure) are analyzed by RT-PCR. Probe PF-CBP1 moderately reduces LPS-induced IL-6 and IFN-β expression at 10 μM, and a decrease in IL-1β expression is evident at 3 μM. (Only for Reference) |
分子量 | 488.62 |
分子式 | C29H36N4O3 |
CAS No. | 1962928-21-7 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 50 mg/mL (102.33 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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