For research use only.

Catalog No.S7315

6 publications

PFI-3 Chemical Structure

Molecular Weight(MW): 321.37

PFI-3 is a selective chemical probe for SMARCA bromodomains, including SMARCA2, SMARCA4 and PB1(5) bromodomains.

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Selleck's PFI-3 has been cited by 6 publications

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  • Western blot analysis of Brg1, α-SMA and Col1a1 expression in the presence of PFI-3(0uM, 5uM, 10uM,20uM,40uM,80uM) for 48 h in the indicated concentration in LX-2 cells.

    Exp Cell Res, 2018, 364(2):191-197. PFI-3 purchased from Selleck.

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Biological Activity

Description PFI-3 is a selective chemical probe for SMARCA bromodomains, including SMARCA2, SMARCA4 and PB1(5) bromodomains.
PB1(5) bromodomains [1] SMARCA4 [4]
(Cell-free assay)
(Cell-free assay)
(Cell-free assay)
55 nM(Kd) 72 nM(Kd) 110 nM(Kd)
In vitro

PFI-3 shows a significant selectivity for PB1(5) and SMARCA2/4 over 36 other tested kinases[1]. PFI-3 is a potent and cell active protein interaction inhibitor that selectively binds to essential BAF bromodomains. PFI-3 is screened in a commercial screening panel comprising 102 cellular receptors as well as 30 enzyme assays, revealing only interactions against four GPCRs with micromolar affinity and no significant additional interactions outside the BRD family, confirming its excellent broader pharmacological selectivity. Stability measurements confirmed that PFI-3 has a half-life in aqueous solutions exceeding 7 days at 37°C. In long-term experiments, PFI-3 significantly altered gene expression programs that are important for differentiation of stem cells. PFI-3 mimics the effect of Brg1 deletion, resulting in an increase of the repressive H3K27me3 mark at the TSSs and Stat3 binding sites of these genes[2]. PFI-3 has a half-life of >250 h in PBS, pH 7.4, at 20 °C[3].

Methods Test Index PMID

PubMed: 26139243     

In situ cell extraction of Hela cells expressing GFP-tagged SMARCA2 bromodomain (green) co-treated with SAHA (5 μM) and PFI-3 (or DMSO control) for 2 hours with Hoescht nuclear counterstain (red). Hela control cells expressing GFP-tagged BRD4 treated (2 hours) with JQ1. 



Cell Research:


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  • Cell lines: trophoblast stem cells
  • Concentrations: 2 μM
  • Incubation Time: 24 h
  • Method:

    TSC are cultured in stemness or differentiation conditions and treated with 2 μM PFI-3 or 10 μM control compound or indicated concentrations for 24 hours or during the entire differentiation induction (4 days), respectively. In case of the differentiation samples, the PFI-3 or control compound exposure started 1 day before the induction of differentiation. RNA was isolated as for the ESC samples.

    (Only for Reference)

Solubility (25°C)

In vitro DMSO 64 mg/mL (199.14 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 321.37


CAS No. 1819363-80-8
Storage powder
in solvent
Synonyms N/A
Smiles OC1=CC=CC=C1C(=O)\C=C\N2CC3CC2CN3C4=NC=CC=C4

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Epigenetic Reader Domain Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID