PFI-3

Catalog No.S7315

For research use only.

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

PFI-3 Chemical Structure

CAS No. 1819363-80-8

Selleck's PFI-3 has been cited by 10 Publications

1 Customer Review

Purity & Quality Control

Choose Selective Epigenetic Reader Domain Inhibitors

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

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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BL21(DE3)-R3-pRARE2 NVji[FJ6TnWwY4Tpc44h[XO|YYm= M4DxSmJqdmSrbnegZYZncW6rdImgeI8hUGm|Nj30ZYdo\WRiaIXtZY4hemWlb33ibY5idnRiUFKxJIJzd22xZH;tZYlvKGm|b3\vdo0hPSCneIDy[ZN{\WRiaX6gSZNkcGW{aXPobYEh[2:uaTDCUFIyMESHMzmtVlMueFKDUlWyJINmdGy|IHL5JHZRNUmWQzDtbYNzd2OjbH;ybY1mfHK7LDDL[F0xNjB2ON88US=> NETsPYw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{GxPVYzPid-MkexNVk3OjZ:L3G+
BL21(DE3)-R3-pRARE2 MnzmSpVv[3Srb36gZZN{[Xl? M2K1RmJqdmSrbnegZYZncW6rdImgeI8hUGm|Nj30ZYdo\WRiaIXtZY4hemWlb33ibY5idnRiU13BVmNCPCCkcn;tc4RwdWGrbjDlfJBz\XO|ZXSgbY4hTXOlaHXybYNpcWFiY3;sbUBDVDJzKFTFN{kuWjNvcGLBVmUzKGOnbHzzJIJ6KF[SLVnUR{BucWO{b3PhcI9zcW2ndIL5MEBM\D1yLkC4Pe69VQ>? M4LIblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUG5OlI3Lz5{N{GxPVYzPjxxYU6=
BL21 (DE3)-R3-BirA NWLydGNHTnWwY4Tpc44h[XO|YYm= MYrCbY5lcW6pIHHm[olvcXS7IITvJIh2dWGwIGDCNUBqe2:ob4LtJFUh\XiycnXzd4VlKGmwIFLMNlEhMESHMzmtVlMuSmm{QTDj[YxteyCkeTDpd491cGW{bXHsJJRqfHKjdHnvckBk[Wyxcnnt[ZRzgSxiS3S8NE4y|ryP NXXVUGsxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexNVU2PTVpPkK3NVE2PTV3PD;hQi=>
BL21 (DE3)-R3-BirA MU\GeY5kfGmxbjDhd5NigQ>? MXzCbY5lcW6pIHHm[olvcXS7IITvJIh2dWGwIGPNRXJESTRiZYjwdoV{e2WmIHnuJGJNOjFiKFTFN{kuWjNvQnnyRUBk\WyuczDifUBqe2:2aHXycYFtKHSrdILheIlwdiClYXzvdolu\XS{eTygT4Q9OC5zzszN MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzFzNUW1OUc,OjdzMUW1OVU9N2F-
C2C12 MX7GeY5kfGmxbjDhd5NigQ>? NGLPRoo2ODBibl2geI8hPTBidV2= MX3Jcohq[mm2aX;uJI9nKGSrZn\ldoVvfGmjdHnvckBqdiCvb4Xz[UBEOkNzMjDj[YxteyCjc4Pld5Nm\CCjczDzbI9zfGWwaX7nJI9nKG27b4T1ZoV{KHerdHigcI94\XJiboXjcIVqKGG2IEWwNEBvVSC2bzC1NEB2VSCkeTDIVnAueGW{b4jp[IF{\S2kYYPl[EBqdW23bn;jfZRw[2inbXnzeJJ6KHKnbHH0bZZmKHSxIHPvcpRzd2x? MlvhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzMUW1OVUoRjJ5MUG1OVU2RC:jPh?=
C2C12 M1zUfGZ2dmO2aX;uJIF{e2G7 M{X1PVEhfU1? M{TlWGlvcGmkaYTpc44hd2ZiZHnm[oVz\W62aXH0bY9vKGmwIH3veZNmKEN{Q{GyJINmdGy|IHHzd4V{e2WmIHHzJJN2eHC{ZYPzbY9vKG:oIF35TGMh\XiycnXzd4lwdiCjdDCxJJVOKGK7IFjSVE1x\XKxeHnkZZNmNWKjc3XkJIludXWwb3P5eI9kcGWvaYP0dpk> MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzFzNUW1OUc,OjdzMUW1OVU9N2F-
C3H10T1/2 NF36eIZHfW6ldHnvckBie3OjeR?= MYmxJJVO Mo\nTY5pcWKrdHnvckBw\iCmaX\m[ZJmdnSrYYTpc44hd2ZibX;1d4UhSzOKMUDUNU8zKGOnbHzzJJRwKGGmaYDvZ5l1\XNiYYPz[ZN{\WRiYYOgcIlxcWRiYXPjeY12dGG2aX;uJIF1KDFidV2gZpkhd2muIILl[EBQKHO2YXnubY5oNWKjc3XkJIF{e2G7 MljpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzMUW1OVUoRjJ5MUG1OVU2RC:jPh?=
C3H10T1/2 Mof3SpVv[3Srb36gZZN{[Xl? MWmyNEB2VQ>? MnzCTY5pcWKrdHnvckBw\iCmaX\m[ZJmdnSrYYTpc44hd2ZibX;1d4UhSzOKMUDUNU8zKGOnbHzzJJRwKGGmaYDvZ5l1\XNiYYPz[ZN{\WRiYYOgcIlxcWRiYXPjeY12dGG2aX;uJIF1KDJyIIXNJIJ6KG:rbDDy[YQhVyC|dHHpcolv\y2kYYPl[EBie3OjeR?= NYHaeI1DRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexNVU2PTVpPkK3NVE2PTV3PD;hQi=>
Assay
Methods Test Index PMID
Immunofluorescence SMARCA2 BRD 26139243

Protocol (from reference)

Cell Research:

[2]

  • 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.

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 321.37
Formula

C19H19N3O2

CAS No. 1819363-80-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1C2CN(C1CN2C3=CC=CC=N3)C=CC(=O)C4=CC=CC=C4O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy PFI-3 | PFI-3 supplier | purchase PFI-3 | PFI-3 cost | PFI-3 manufacturer | order PFI-3 | PFI-3 distributor