Home Epigenetics Epigenetic Reader Domain inhibitor PFI-3 For research use only.

PFI-3

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

PFI-3 Chemical Structure

PFI-3 Chemical Structure

CAS No. 1819363-80-8

Purity & Quality Control

PFI-3 Related Products

Signaling Pathway

Epigenetic Reader Domain Signaling Pathways

Epigenetic Reader Domain Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BL21(DE3)-R3-pRARE2 Function assay Binding affinity to His6-tagged human recombinant PB1 bromodomain isoform 5 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by VP-ITC microcalorimetry, Kd=0.048μM 27119626
BL21(DE3)-R3-pRARE2 Function assay Binding affinity to His6-tagged human recombinant SMARCA4 bromodomain expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by VP-ITC microcalorimetry, Kd=0.089μM 27119626
BL21 (DE3)-R3-BirA Function assay Binding affinity to human PB1 isoform 5 expressed in BL21 (DE3)-R3-BirA cells by isothermal titration calorimetry, Kd<0.1μM 27115555
BL21 (DE3)-R3-BirA Function assay Binding affinity to human SMARCA4 expressed in BL21 (DE3)-R3-BirA cells by isothermal titration calorimetry, Kd<0.1μM 27115555
C2C12 Function assay 500 nM to 50 uM Inhibition of differentiation in mouse C2C12 cells assessed as shortening of myotubes with lower nuclei at 500 nM to 50 uM by HRP-peroxidase-based immunocytochemistry relative to control 27115555
C2C12 Function assay 1 uM Inhibition of differentiation in mouse C2C12 cells assessed as suppression of MyHC expression at 1 uM by HRP-peroxidase-based immunocytochemistry 27115555
C3H10T1/2 Function assay 1 uM Inhibition of differentiation of mouse C3H10T1/2 cells to adipocytes assessed as lipid accumulation at 1 uM by oil red O staining-based assay 27115555
C3H10T1/2 Function assay 20 uM Inhibition of differentiation of mouse C3H10T1/2 cells to adipocytes assessed as lipid accumulation at 20 uM by oil red O staining-based assay 27115555
Click to View More Cell Line Experimental Data

Biological Activity

Description PFI-3 is a selective chemical probe for SMARCA bromodomains, including SMARCA2, SMARCA4 and PB1(5) bromodomains.
Targets
PB1(5) bromodomains [1] SMARCA4 [4]
(Cell-free assay)		 SMARCA2B [4]
(Cell-free assay)		 SMARCA2A [4]
(Cell-free assay)
55 nM(Kd) 72 nM(Kd) 110 nM(Kd)
In vitro
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].
Cell Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Immunofluorescence SMARCA2 BRD 26139243

Chemical Information & Solubility

Molecular Weight 321.37 Formula

C19H19N3O2
CAS No. 1819363-80-8 SDF Download PFI-3 SDF
Smiles C1C2CN(C1CN2C3=CC=CC=N3)C=CC(=O)C4=CC=CC=C4O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 64 mg/mL ( (199.14 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

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.

Handling Instructions

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