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PF CBP1

Names

[ CAS No. ]:
1962928-21-7

[ Name ]:
PF CBP1

[Synonym ]:
5-(3,5-Dimethyl-1,2-oxazol-4-yl)-1-[2-(4-morpholinyl)ethyl]-2-[2-(4-propoxyphenyl)ethyl]-1H-benzimidazole
1H-Benzimidazole, 5-(3,5-dimethyl-4-isoxazolyl)-1-[2-(4-morpholinyl)ethyl]-2-[2-(4-propoxyphenyl)ethyl]-

Biological Activity

[Description]:

PF-CBP1 is a highly selective inhibitor of the CREB binding protein bromodomain[1].

[Related Catalog]:

Research Areas >> Neurological Disease
Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

[In Vitro]

PF-CBP1 modulates key inflammatory genes in primary macrophages. PF-CBP1 downregulates RGS4 in neurons, a target linked to Parkinson's disease. PF-CBP1 is 139-fold selective over BRD4 in the biochemical assays and >105-fold selective by ITC. F-CBP1 is also a potent inhibitor of EP300 (a result observed for other CBP inhibitors[1].

[References]

[1]. Chekler EL, et al. Transcriptional Profiling of a Selective CREB Binding Protein Bromodomain Inhibitor Highlights Therapeutic Opportunities. Chem Biol. 2015 Dec 17;22(12):1588-96.

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
673.5±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C29H36N4O3

[ Molecular Weight ]:
488.621

[ Flash Point ]:
361.1±31.5 °C

[ Exact Mass ]:
488.278748

[ LogP ]:
5.46

[ Vapour Pressure ]:
0.0±2.1 mmHg at 25°C

[ Index of Refraction ]:
1.615

[ Storage condition ]:
-20℃

Related Compounds