PF-CBP1 HCl - 10mM in DMSO , CAS No.2070014-93-4

CAS: 2070014-93-4 Cat. No.: P422510 Fórmula: C₂₉H₃₇ClN₄O₃ Peso molecular: 525.08 PubChem CID: 119081416

GRADE & PURITY 10mM in DMSO

Synonyms

5-(Dimethyl-1,2-oxazol-4-yl)-1-[2-(morpholin-4-yl)ethyl]-2-[2-(4-propoxyphenyl)ethyl]-1H-1,3-benzodiazole hydrochloride

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Visão geral

Information

PF-CBP1 HCl PF-CBP1 HCl is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP) .It inhibits CREBBP and p300 bromodomains with IC50 of 125 and 363 nM respectively.

Targets

CREBBP (Cell-free assay); p300/CBP (Cell-free assay) 125nM; 363nM

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(from reference)

Cell lines：mouse J774 macrophage-like cell line 

Concentrations：0.1-10\xa0μM 

Incubation Time：30min 

Specifications

Sinónimos

5-(Dimethyl-1,2-oxazol-4-yl)-1-[2-(morpholin-4-yl)ethyl]-2-[2-(4-propoxyphenyl)ethyl]-1H-1,3-benzodiazole hydrochloride

Especificações e pureza

10mM in DMSO

Mecanismos bioquímicos e fisiológicos

PF-CBP1 HCl is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP).It inhibits CREBBP and p300 bromodomains with IC50 of 125 and 363 nM respectively.

Condições de armazenamento de armazenamento

Store at -80°C

Enviado em

Dry ice packs + Cold packs

Este produto requer transporte de cadeia fria. Serviços terrestres e outros serviços econômicos não estão disponíveis.

Tipo de ação

INHIBITOR

Nomes e identificadores

Pubchem Sid

528766625

Sorrisos canónicos

CCCOC1=CC=C(C=C1)CCC2=NC3=C(N2CCN4CCOCC4)C=CC(=C3)C5=C(ON=C5C)C.Cl

IUPAC Name

4-[2-[5-(3,5-dimethyl-1,2-oxazol-4-yl)-2-[2-(4-propoxyphenyl)ethyl]benzimidazol-1-yl]ethyl]morpholine;hydrochloride

InChIKey

HFOZCHHWLMTUTP-UHFFFAOYSA-N

INCHI

1S/C29H36N4O3.ClH/c1-4-17-35-25-9-5-23(6-10-25)7-12-28-30-26-20-24(29-21(2)31-36-22(29)3)8-11-27(26)33(28)14-13-32-15-18-34-19-16-32;/h5-6,8-11,20H,4,7,12-19H2,1-3H3;1H

PubChem CID

119081416

Peso molecular

525.08

Propriedades químicas e físicas

• Peso molecular: 525.100 g/mol
• Hydrogen Bond Donor Count: 1
• Hydrogen Bond Acceptor Count: 6
• Rotatable Bond Count: 10
• Exact Mass: 524.255 Da
• Monoisotopic Mass: 524.255 Da
• Topological Polar Surface Area: 65.600 Ų
• Heavy Atom Count: 37
• Formal Charge: 0
• Complexity: 654.000
• Isotope Atom Count: 0
• Defined Atom Stereocenter Count: 0
• Undefined Atom Stereocenter Count: 0
• Defined Bond Stereocenter Count: 0
• Undefined Bond Stereocenter Count: 0
• The total count of all stereochemical bonds: 0
• Covalently-Bonded Unit Count: 2

XLogP3