Home Epigenetics Epigenetic Reader Domain inhibitor PF-CBP1 HCl For research use only.

PF-CBP1 HCl

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.

PF-CBP1 HCl Chemical Structure

PF-CBP1 HCl Chemical Structure

CAS: 2070014-93-4

Selleck's PF-CBP1 HCl has been cited by 4 publications

Purity & Quality Control

Batch: S818001 DMSO] 100 mg/mL] false] Ethanol] 100 mg/mL] false] Water] Insoluble] false Purity: 99.99%
99.99

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Biological Activity

Description 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.
Targets
CREBBP [1]
(Cell-free assay)		 p300/CBP [1]
(Cell-free assay)
125nM 363nM
In vitro
In vitro 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].
Cell Research Cell lines mouse J774 macrophage-like cell line
Concentrations 0.1-10 μM
Incubation Time 30min
Method

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. 

Chemical Information & Solubility

Molecular Weight 525.08 Formula

C29H36N4O3.HCl
CAS No. 2070014-93-4 SDF Download PF-CBP1 HCl SDF
Smiles CCCOC1=CC=C(C=C1)CCC2=NC3=C(N2CCN4CCOCC4)C=CC(=C3)C5=C(ON=C5C)C.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (190.44 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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