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PF-CBP1 (hydrochloride)

Product Name
PF-CBP1 (hydrochloride)
CAS No.
2070014-93-4
Chemical Name
PF-CBP1 (hydrochloride)
Synonyms
PF-CBP1 (hydrochloride);PF-CBP1 hydrochloride(b);HFOZCHHWLMTUTP-UHFFFAOYSA-N;4-[2-[5-(3,5-dimethylisoxazol-4-yl)-2-[2-(4-propoxyphenyl)ethyl]benzimidazol-1-yl]ethyl]morpholine;5-(3,5-dimethyl-1,2-oxazol-4-yl)-1-[2-(morpholin-4-yl)ethyl]-2-[2-(4-propoxyphenyl)ethyl]-1H-1,3-benzodiazole;5-?(3,?5-Dimethyl-?4-?isoxazolyl)?-?1-?[2-?(4-?morpholinyl)?ethyl]?-?2-?[2-?(4-?propoxyphenyl)?ethyl]?-1H-?benzimidazole Hydrochloride;parkinson's disease,HATs,cortical,inflammatory,HAT,Histone Acetyltransferase,PF CBP1 hydrochloride,inhibit,RGS4,epilepsy,Epigenetic Reader Domain,PF-CBP1,PFCBP1 hydrochloride,Inhibitor,neurological disorder,PF-CBP-1 hydrochloride,neuron
CBNumber
CB33122348
Molecular Formula
C29H37ClN4O3
Formula Weight
525.09
MOL File
2070014-93-4.mol
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PF-CBP1 (hydrochloride) Property

storage temp. 
Store at -20°C
solubility 
≥52.5 mg/mL in DMSO; insoluble in H2O; ≥40.6 mg/mL in EtOH
form 
solid
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

TRC
Product number
D456460
Product name
5-​(3,​5-Dimethyl-​4-​isoxazolyl)​-​1-​[2-​(4-​morpholinyl)​ethyl]​-​2-​[2-​(4-​propoxyphenyl)​ethyl]​-1H-​benzimidazoleHydrochloride
Packaging
1mg
Price
$45
Updated
2021/12/16
ChemScene
Product number
CS-5546
Product name
PF-CBP1hydrochloride
Purity
99.85%
Packaging
5mg
Price
$50
Updated
2021/12/16
ApexBio Technology
Product number
B6197
Product name
PF-CBP1hydrochloride
Packaging
10mg
Price
$75
Updated
2021/12/16
ChemScene
Product number
CS-5546
Product name
PF-CBP1hydrochloride
Purity
99.85%
Packaging
10mg
Price
$75
Updated
2021/12/16
ChemScene
Product number
CS-5546
Product name
PF-CBP1hydrochloride
Purity
99.85%
Packaging
25mg
Price
$150
Updated
2021/12/16
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PF-CBP1 (hydrochloride) Chemical Properties,Usage,Production

Uses

5-?(3,?5-Dimethyl-?4-?isoxazolyl)?-?1-?[2-?(4-?morpholinyl)?ethyl]?-?2-?[2-?(4-?propoxyphenyl)?ethyl]?-1H-?benzimidazole Hydrochloride is a potent and selective bromodomain of CREB binding protein (CBP BRD) inhibitor. 5-?(3,?5-Dimethyl-?4-?isoxazolyl)?-?1-?[2-?(4-?morpholinyl)?ethyl]?-?2-?[2-?(4-?propoxyphenyl)?ethyl]?-1H-?benzimidazole Hydrochloride downregulates inflammatory genes in macrophages and has therapeutic potential for treating neurological disorders.

Biological Activity

pf-cbp1 is a cbp/p300 bromodomain inhibitor.bromodomains are reported to be involved in transcriptional regulation via the recognition of acetyl lysine modifications. however, selective bromodomain modulators are still lacking, though the hydrophobic pocket makes bromodomains attractive targets.

in vitro

pf-cbp1 showed a significant reduction in brd4 potency, while retained cbp affinity. in order to evaluate compound-related cytotoxicity during gene transcription, primary macrophages were stimulated with lps and were further analyzed to determine the cell viability. results showed that pf-cbp1 and the negative control isox-inact did not cause cytotoxicity even at high concentrations up to 30 mm. in addition, pf-cbp1 at 10 mm was able to moderately reduce lps-induced il-6 and ifn-b expression, and a decrease in il-1b expression was observed at 3 mm. moreover, the rat primary cortical neurons were treated with pf-cbp1, vehicle, or the negative control isox-inact, and the results showed that at 1 hr, there were no changes in rgs4 expression compared with vehicle. however, the treatment of pf-cbp1 at 10-fold ic50 dose could significantly reduce rgs4 mrna levels at 24 hr when compared with that of vehicle [1].

IC 50

125 and 363 nm for crebbp and p300 bromodomain, respectively

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.

PF-CBP1 (hydrochloride) Preparation Products And Raw materials

Raw materials

Preparation Products

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PF-CBP1 (hydrochloride) Suppliers

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2070014-93-4, PF-CBP1 (hydrochloride)Related Search:


  • PF-CBP1 (hydrochloride)
  • HFOZCHHWLMTUTP-UHFFFAOYSA-N
  • 5-(3,5-dimethyl-1,2-oxazol-4-yl)-1-[2-(morpholin-4-yl)ethyl]-2-[2-(4-propoxyphenyl)ethyl]-1H-1,3-benzodiazole
  • 5-?(3,?5-Dimethyl-?4-?isoxazolyl)?-?1-?[2-?(4-?morpholinyl)?ethyl]?-?2-?[2-?(4-?propoxyphenyl)?ethyl]?-1H-?benzimidazole Hydrochloride
  • 4-[2-[5-(3,5-dimethylisoxazol-4-yl)-2-[2-(4-propoxyphenyl)ethyl]benzimidazol-1-yl]ethyl]morpholine
  • parkinson's disease,HATs,cortical,inflammatory,HAT,Histone Acetyltransferase,PF CBP1 hydrochloride,inhibit,RGS4,epilepsy,Epigenetic Reader Domain,PF-CBP1,PFCBP1 hydrochloride,Inhibitor,neurological disorder,PF-CBP-1 hydrochloride,neuron
  • PF-CBP1 hydrochloride(b)
  • 2070014-93-4
  • C29H37ClN4O3