Home Epigenetics Histone Methyltransferase inhibitor - SETD inhibitor PFI-2 HCl For research use only.

PFI-2 HCl

PFI-2 is a potent, selective, and cell-active lysine methyltransferase SETD7 inhibitor with Ki (app) and IC50 of 0.33 nM and 2 nM, 1000-fold selectivity over other methyltransferases and other non-epigenetic targets.

PFI-2 HCl Chemical Structure

PFI-2 HCl Chemical Structure

CAS No. 1627607-87-7

Purity & Quality Control

PFI-2 HCl Related Products

Signaling Pathway

Histone Methyltransferase Signaling Pathways

Histone Methyltransferase Signaling Pathway

Biological Activity

Description PFI-2 is a potent, selective, and cell-active lysine methyltransferase SETD7 inhibitor with Ki (app) and IC50 of 0.33 nM and 2 nM, 1000-fold selectivity over other methyltransferases and other non-epigenetic targets.
Targets
SETD7 [1]
(Cell-free assay)		 SETD7 [1]
(Cell-free assay)
0.33 nM(Ki) 2 nM
In vitro
In vitro (R)-PFI-2 shows 500-fold more inhibitory activity against human SETD7 than its enantiomer, (S)-PFI-2. In a cellular environment, through direct interactions with SETD7, affects Yes-Associated protein localization and phenocopies Setd7 genetic deletion on Hippo pathway signaling. [1]

Chemical Information & Solubility

Molecular Weight 535.98 Formula

C23H25F4N3O3S.HCl
CAS No. 1627607-87-7 SDF Download PFI-2 HCl SDF
Smiles C1CCN(C1)C(=O)C(CC2=CC(=CC=C2)C(F)(F)F)NS(=O)(=O)C3=CC4=C(CNCC4)C(=C3)F.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 99 mg/mL ( (184.7 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 66 mg/mL

Water : 4 mg/mL


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In vivo
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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.
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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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