A chemical probe that specifically binds to the bromodomain of BRPF1 (Kd = 13 nM)

PFI-4 – 5 mg

Brand:
Cayman
CAS:
900305-37-5
Storage:
-20
UN-No:
Non-Hazardous - /

The bromodomain and PHD finger-containing (BRPF) proteins are scaffolding components of chromatin-binding MOZ/MORF histone acetyltransferase complexes, which have activity as transcriptional regulators.{21051,29177} BRPF1, aka BR140 or Peregrin, is important for maintaining Hox gene expression and the development of multiple tissues, axial skeleton, and the hematopoietic system.{29177} PFI-4 is a chemical probe that specifically binds to the bromodomain of BRPF1 (Kd = 13 nM), inhibiting binding to tri-acetylated histone 4 (residues 1-21).{29176} It has much lower affinity for bromodomain 1 of BRD4 (Kd = >50 µM) and is selective for BRPF1 over BRPF2 and BRPF3.{29176} PFI-4 is potent in cells, with an IC50 value of 250 nM. See the Structural Genomics Consortium (SGC) website for more information.  

 

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Description

A chemical probe that specifically binds to the bromodomain of BRPF1 (Kd = 13 nM), inhibiting binding to tri-acetylated histone 4 (residues 1-21); potent in cells, with an IC50 value of 250 nM

Formal name: N-[2,3-dihydro-1,3-dimethyl-2-oxo-6-(1-pyrrolidinyl)-1H-benzimidazol-5-yl]-2-methoxy benzamide

Synonyms: 

Molecular weight: 380.4

CAS: 900305-37-5

Purity: ≥98%

Formulation:

Product Type|Biochemicals|Small Molecule Inhibitors|Chromatin Reader Interactions||Research Area|Epigenetics, Transcription, & Translation|Readers|Bromodomains

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