Home Epigenetics Epigenetic Reader Domain inhibitor PF-CBP1 HCl

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PF-CBP1 HCl Epigenetic Reader Domain inhibitor

Cat.No.S8180

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 Epigenetic Reader Domain inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 525.08

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 525.08 Formula

C29H36N4O3.HCl

 Storage (From the date of receipt)
CAS No. 2070014-93-4 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CCCOC1=CC=C(C=C1)CCC2=NC3=C(N2CCN4CCOCC4)C=CC(=C3)C5=C(ON=C5C)C.Cl

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (190.44 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
CREBBP [1]
(Cell-free assay)
125nM
p300/CBP [1]
(Cell-free assay)
363nM
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].
References

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