General
Preferred name
PFI-4
Synonyms
PFI 4 ()
PFI4 ()
GSK6853 ()
P&D ID
PD000017
CAS
900305-37-5
Tags
available
drug candidate
probe
Drug indication
Discovery agent
Probe info
Probe type
experimental probe
P&D approved
Probe selectivity
protein-selective
Probe sources
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
Probe control not defined
Orthogonal probes
4
No orthogonal probes found
Similar probes
2
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
This compound from the Structural Genomics Consortium's (SGC) Epigenetics Probes Collection, is a useful tool for studying the function of the bromodomain-containing protein, BRPF1. BRPF proteins 1, 2 and 3 provide the scaffold for the formation of MYST complexes which play essential functions in DNA repair, recombination, replication and activation of transcription. PFI-4 is selective for the BRPF1B isoform. The BRPF1A isoform contains an amino acid insertion which prevents its binding to acetylated histone peptides.
(GtoPdb)
DESCRIPTION
PFI-4 (compound 11) is a potent and highly selective BRPF1 Bromodomain (BRPF1B) inhibitor, with an IC50 of 172 nM. PFI-4 can be used to explore the functional mechanisms of the HBO1/BRPF1 complex and to study bone loss and osteolytic malignant bone lesions[1][2].
PRICE
52
MOA
Inhibitor
(Chemical Probes.org)
DESCRIPTION
Potent and selective BRD9 and BRD7 inhibitor; orally active
(Tocris Bioactive Compound Library)
DESCRIPTION
Potent and selective BRPF1 bromodomain inhibitor
(Tocriscreen Plus)
DESCRIPTION
PFI-4 is a potent and highly selective BRPF1 inhibitor, with an IC50 of 47 nM. PFI-4 can be used to explore the functional mechanisms of the HBO1/BRPF1 complex and to study bone loss and osteolytic malignant bone lesions.
(Enamine Bioactive Compounds)
DESCRIPTION
PFI-4 is a potent and selective and cell-permeable BRPF1 bromodomain inhibitor.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
18
Bromodomains chemical toolbox
Cayman Chemical Bioactives
Chemical Probes.org
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugMAP
Enamine Bioactive Compounds
EU-OPENSCREEN Bioactive Compound Library
EUbOPEN Chemogenomics Library
Guide to Pharmacology
High-quality chemical probes
MedChem Express Bioactive Compound Library
Novartis Chemogenetic Library (NIBR MoA Box)
Selleckchem Bioactive Compound Library
SGC Probes
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Plus
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
14
Molecular Weight
380.18
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
1
Rotatable Bonds
4
Ring Count
4
Aromatic Ring Count
3
cLogP
2.74
TPSA
68.5
Fraction CSP3
0.33
Chiral centers
0.0
Largest ring
6.0
QED
0.76
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target Type
Cell Biology
Target
BRPF1
BRPF2
BRPF3
Epigenetic Reader Domain
Primary Target
Bromodomains
MOA
Inhibitor
BRPF1B
BRPF1B inhibitor
Bromodomain inhibitor
Member status
member
Pathway
Epigenetics
Chromatin/Epigenetic
Target class
Epigenetic
Target subclass
Bromodomain
Recommended Cell Concentration
1 uM
Source data
