PZ0325
PF-CBP1
≥98% (HPLC)
Synonym(s):
4-(2-(5-(3,5-Dimethylisoxazol-4-yl)-2-(4-propoxyphenethyl)-1H-benzo[d]imidazol-1-yl)ethyl)morpholine, 5-(Dimethyl-1,2-oxazol-4-yl)-1-[2-(morpholin-4-yl)ethyl]-2-[2-(4-propoxyphenyl)ethyl]-1H-1,3-benzodiazole, PF CBP1, PF-06670910
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About This Item
Empirical Formula (Hill Notation):
C29H36N4O3
Molecular Weight:
488.62
UNSPSC Code:
12352200
NACRES:
NA.77
Quality Level
Assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 20 mg/mL, clear
storage temp.
room temp
General description
The gene CBP (CREB binding protein) is mapped to human chromosome 16p13.
Biochem/physiol Actions
CBP is a transcriptional coactivator. The protein is a link between the DNA-associated transcription factors and the RNA polymerase 2 complex. It also exhibits histone acetyltransferase activity.
PF-CBP1 is potent and highly-selective inhibitor of the bromodomain of CREB binding protein (CBP BRD) that down regulates targets of CBP in macrophages primary neurons. Also, PF-CBP1 significantly reduces levels of RGS4 mRNA levels in neurons.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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Natalie H Theodoulou et al.
ChemMedChem, 11(5), 477-487 (2016-01-11)
The bromodomain and extra terminal (BET) family of bromodomains have been the focus of extensive research, leading to the development of many potent, selective chemical probes and recent clinical assets. The profound biology associated with BET bromodomain inhibition has provided
Kunka Kamenarova et al.
Human pathology, 47(1), 144-149 (2015-11-26)
Rubinstein-Taybi syndrome (RSTS) is a rare autosomal dominant congenital disorder (prevalence, 1:125000-720000) characterized by broad thumbs and halluces, facial dysmorphism, psychomotor development delay, skeletal defects, abnormalities in the posterior fossa, and short stature. The purpose of this study was to
Spontaneous complete and sustained remission of a rearrangement CBP (16p13)-positive disseminated congenital myelosarcoma.
Carl Friedrich Classen et al.
Annals of hematology, 84(4), 274-275 (2004-12-18)
Eugene L Piatnitski Chekler et al.
Chemistry & biology, 22(12), 1588-1596 (2015-12-17)
Bromodomains are involved in transcriptional regulation through the recognition of acetyl lysine modifications on diverse proteins. Selective pharmacological modulators of bromodomains are lacking, although the largely hydrophobic nature of the pocket makes these modules attractive targets for small-molecule inhibitors. This
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