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PF-CBP1

Catalog No. T3973   CAS 1962928-21-7

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).

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PF-CBP1 Chemical Structure
PF-CBP1, CAS 1962928-21-7
Pack Size Availability Price/USD Quantity
1 mg In stock $ 37.00
2 mg In stock $ 50.00
5 mg In stock $ 63.00
10 mg In stock $ 110.00
25 mg In stock $ 216.00
50 mg In stock $ 391.00
100 mg In stock $ 582.00
1 mL * 10 mM (in DMSO) In stock $ 63.00
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Purity: 99.91%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description 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).
Targets&IC50 p300 BD:363 nM, CREBBP:125 nM
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.
Cell Research 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)
Molecular Weight 488.62
Formula C29H36N4O3
CAS No. 1962928-21-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL

TargetMolReferences and Literature

1. Eugene L, et al. Chem Biol. 2015, 22(12):1588-1596.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Highly Selective Inhibitor Library Histone Modification Compound Library Epigenetics Compound Library Bioactive Compound Library Bioactive Compounds Library Max NO PAINS Compound Library PPI Inhibitor Library

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Keywords

PF-CBP1 1962928-21-7 Chromatin/Epigenetic Epigenetic Reader Domain PFCBP1 PF-CBP-1 Inhibitor PF CBP1 inhibit inhibitor

 

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