首页Chromatin/EpigeneticEpigenetic Reader DomainPF-CBP1
PF-CBP1
编号 T3973    
CAS 1962928-21-7     分子式 C29H36N4O3     分子量 488.63
靶点: CREB;
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).
纯度:98.0%
规格 库存 单价 数量
2 mg 待询 338.00
5 mg 待询 608.00
10 mg 待询 1072.00
25 mg 待询 2096.00
50 mg 待询 3792.00
100 mg 待询 6728.00
1 mL * 10 mM (in DMSO) 待询 608.00
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生物活性

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

CREB,

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.

体内活性

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)

细胞系: mouse J774 macrophage-like cell line

化学信息

分子量

488.63

分子式

C29H36N4O3

CAS

1962928-21-7

溶解度

DMSO: 100 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

store at -80°C

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 2.047 ml 10.233 ml 20.465 ml
5 mM 0.409 ml 2.047 ml 4.093 ml
10 mM 0.205 ml 1.023 ml 2.047 ml
50 mM 0.041 ml 0.205 ml 0.409 ml
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