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PF-CBP1,CBP/p300BromodomainInhibitor

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产品名称: PF-CBP1,CBP/p300BromodomainInhibitor
产品型号: M60313-2s
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简单介绍

PF-CBP1,CBP/p300BromodomainInhibitor


PF-CBP1,CBP/p300BromodomainInhibitor  的详细介绍
Product Information
Molecular Weight: 488.62
Formula: C29H36N4O3
Purity: ≥98%
CAS#: n/a
Solubility: DMSO up to 100 mM; EtOH up to 100 mM
Chemical Name: 4-(2-(5-(3,5-dimethylisoxazol-4-yl)-2-(4-propoxyphenethyl)-1H-benzo[d]imidazol-1-yl)ethyl)morpholine
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

PF-CBP1 is a potent and selective CBP/p300 bromodomain inhibitor (IC50 ~125 nM for CBP and 363 nM for p300). It has >100-fold selectivity for CBP over BRD4, and shows selectivity over a panel of other bromodomains. PF-CBP1 reduces LPS-induced IL-1β, IL-6 and IFN-β expression in macrophages in vitro. It can also downregulate RGS4 expression in primary cortical neurons in vitro.

How to Use:

In vitro:
PF-CBP1 was used at 10 µM final concentration in various assays.
In vivo:
n/a

Reference:


  1. 1. Chekler EL, et al. Transcriptional Profiling of a Selective CREB Binding Protein Bromodomain Inhibitor Highlights Therapeutic Opportunities. (2015) Chem Biol. 22(12):1588-96. 



      
    

  
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