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Chemical Structure| 1819363-80-8 Chemical Structure| 1819363-80-8

Structure of PFI-3
CAS No.: 1819363-80-8

Chemical Structure| 1819363-80-8

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PFI-3 is a potent and selective polybromo 1 and SMARCA4 inhibitor (Kd values are 48 and 89 nM respectively).

Synonyms: PFI-3

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Product Details of PFI-3

CAS No. :1819363-80-8
Formula : C19H19N3O2
M.W : 321.37
SMILES Code : O=C(C1=CC=CC=C1O)/C=C/N2[C@@](C3)([H])CN(C4=NC=CC=C4)[C@@]3([H])C2
Synonyms :
PFI-3
MDL No. :MFCD28100807
InChI Key :INAICWLVUAKEPB-QSTFCLMHSA-N
Pubchem ID :78243717

Safety of PFI-3

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • bromodomain

    SMARCA2A, Kd:72 nM

    SMARCA4, Kd:55 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Ea.hy926 cells 2 μM 24 h PFI-3 significantly decreased TNF-α-induced IL-1β and CCL2 expression PMC7734107
Neural Stem Cells 10 µM 5 days PFI-3 treatment resulted in neurosphere-like formation and loss of self-renewal in neural stem cells. PMC6523874
AdvSca1-SM cells 50 μM 72 h PFI-3 blocked TGF-β1–induced differentiation of AdvSca1-SM cells into myofibroblasts and reduced collagen contraction. PMC10243795
HEK293T cells 5 μM 10 min To evaluate the effect of PFI-3 on translation, results showed that 10-minute inhibition significantly reduced translation levels. PMC9379364
HEK293T cells 5 μM 24 h To evaluate the effect of PFI-3 on translation, results showed that 24-h inhibition significantly reduced translation levels. PMC9379364
neonatal mouse cardiomyocytes 10 μM 24 h After Brg1 inhibition, the protein level of TRPM4 was reduced PMC11669506
Rh30 cells 10 μM 24 h Inhibition of SMARCA4 bromodomain activity increased miR-27a expression. PMC6432638
zebra fish embryos 100 μM 3.5 hpf Inhibit Smarca2 function, accelerate H3K9me3 establishment and chromatin compaction PMC6449393
AdvSca1-SM cells 50 μM 72 h PFI-3 inhibited TGF-β1-induced differentiation of AdvSca1-SM cells into myofibroblasts, reduced the expression of Acta2, Postn, and Mrtfa, and inhibited collagen gel contraction. PMC10243795

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
mice Gli1-CreERT2 ROSA-YFP AdvSca1-SM reporter mice oral gavage 50 mg/kg every 4 days for 4 weeks PFI-3 inhibited the Brg1 bromodomain, reducing injury-induced vascular remodeling and fibrosis. PMC10243795
mice Gli1-CreERT2 ROSA-YFP AdvSca1-SM reporter mice oral gavage 50 mg/kg every 4 days for 4 weeks PFI-3 inhibited the Brg1 bromodomain, reducing pathological vascular remodeling induced by carotid artery ligation, including decreased neointima area, adventitial expansion, and collagen deposition. PMC10243795

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.11mL

0.62mL

0.31mL

15.56mL

3.11mL

1.56mL

31.12mL

6.22mL

3.11mL

References

 

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