An inhibitor of the CBP and p300 bromodomains (IC50s = 125 and 363 nM

PF-CBP1 – 1 mg

Brand:
Cayman
CAS:
1962928-21-7
Storage:
-20
UN-No:
Non-Hazardous - /

CREB-binding protein (CBP) and E1A-associated protein p300 are transcriptional co-activators that modulate DNA replication, DNA repair, cell growth, transformation, and development.{22609,22611} Both CBP and p300 contain bromodomains, which mediate their binding to acetylated lysine residues on histones and other proteins.{21581} PF-CBP1 is an inhibitor of the CBP and p300 bromodomains (IC50s = 125 and 363 nM, respectively).{30310} It displays greater than 100-fold selectivity for the bromodomain of CBP over those of BRD4 and a panel of other proteins.{30310} PF-CBP1 reduces the expression of inflammatory cytokines by LPS-stimulated primary macrophages.{30310} It also suppresses the expression of RGS4 (regulator of G protein signaling 4) in primary cortical neurons.{30310}  

 

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Description

An inhibitor of the CBP and p300 bromodomains (IC50s = 125 and 363 nM, respectively)

Formal name: 5-(3,5-dimethyl-4-isoxazolyl)-1-[2-(4-morpholinyl)ethyl]-2-[2-(4-propoxyphenyl)ethyl]-1H-benzimidazole

Synonyms: 

Molecular weight: 488.6

CAS: 1962928-21-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Chromatin Reader Interactions||Product Type|Biochemicals|Small Molecule Inhibitors|DNA Repair Enzymes||Research Area|Epigenetics, Transcription, & Translation|Readers|Bromodomains||Research Area|Epigenetics, Transcription, & Translation|RNA, DNA, & Protein Synthesis||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Neuroscience

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