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PF-CBP1 hydrochloride (PF-CBP1 HCl) 是 CREB 结合蛋白溴结构域的一种高选择性抑制剂,抑制 CREBBP 和 EP300溴结构域的 IC50分别为 125 和 363 nM。它降低 LPS 诱导的巨噬细胞中炎症因子的表达,也可下调皮质神经元 RGS4 的表达,可用于癫痫和帕金森病等神经疾病的研究。
PF-CBP1 hydrochloride (PF-CBP1 HCl) 是 CREB 结合蛋白溴结构域的一种高选择性抑制剂,抑制 CREBBP 和 EP300溴结构域的 IC50分别为 125 和 363 nM。它降低 LPS 诱导的巨噬细胞中炎症因子的表达,也可下调皮质神经元 RGS4 的表达,可用于癫痫和帕金森病等神经疾病的研究。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 185 | 现货 | |
5 mg | ¥ 413 | 现货 | |
10 mg | ¥ 622 | 现货 | |
25 mg | ¥ 1,230 | 现货 | |
50 mg | ¥ 1,980 | 现货 | |
100 mg | ¥ 3,670 | 现货 | |
200 mg | ¥ 4,770 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 623 | 现货 |
产品描述 | PF-CBP1 hydrochloride (PF-CBP1 HCl) is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP).It inhibits CREBBP and p300 bromodomains with IC50 of 125 and 363 nM respectively. |
靶点活性 | p300/CBP:363nM, CREBBP:125nM |
体外活性 | PF-CBP1 modulates key inflammatory genes in primary macrophages. PF-CBP1 down regulates RGS4 in neurons, a target linked to Parkinson's disease.It is 139-fold selective over BRD4 in the biochemical assays and >105-fold selective by ITC.PF-CBP1 is also a potent inhibitor of EP300 and possesses no cytotoxicity in macrophages, and hepatotoxicity in cell-based models as long as the concentration is not very high[1]. |
别名 | PF-CBP1 HCl |
分子量 | 525.08 |
分子式 | C29H37ClN4O3 |
CAS No. | 2070014-93-4 |
Smiles | Cl.CCCOc1ccc(CCc2nc3cc(ccc3n2CCN2CCOCC2)-c2c(C)noc2C)cc1 |
密度 | no data available |
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: 45 mg/mL (85.7 mM) | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
DMSO
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