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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

    SMARCA4, Kd:55 nM

    SMARCA2A, Kd:72 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 Front Cell Dev Biol. 2020 Nov 30;8:578790.
Neural Stem Cells 10 µM 5 days PFI-3 treatment resulted in neurosphere-like formation and loss of self-renewal in neural stem cells. Stem Cell Reports. 2019 May 14;12(5):1084-1098.
AdvSca1-SM cells 50 μM 72 h PFI-3 blocked TGF-β1–induced differentiation of AdvSca1-SM cells into myofibroblasts and reduced collagen contraction. JCI Insight. 2023 May 8;8(9):e164862.
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. Cancer Res. 2022 Aug 16;82(16):2829-2837.
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. Cancer Res. 2022 Aug 16;82(16):2829-2837.
neonatal mouse cardiomyocytes 10 μM 24 h After Brg1 inhibition, the protein level of TRPM4 was reduced Front Pharmacol. 2024 Dec 12;15:1494205.
Rh30 cells 10 μM 24 h Inhibition of SMARCA4 bromodomain activity increased miR-27a expression. Sci Signal. 2018 Nov 20;11(557):eaau7632.
zebra fish embryos 100 μM 3.5 hpf Inhibit Smarca2 function, accelerate H3K9me3 establishment and chromatin compaction Nat Commun. 2019 Apr 4;10(1):1551.
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. JCI Insight. 2023 May 8;8(9):e164862.

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. JCI Insight. 2023 May 8;8(9):e164862.
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. JCI Insight. 2023 May 8;8(9):e164862.

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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