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PFI-2 HCl Histone Methyltransferase inhibitor

Name: PFI-2 HCl
Brand: Selleck Chemicals
SKU: S7294
Availability: InStock
Rating: 5 (7 reviews)

Cat.No.S7294

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

Chemical Structure

Molecular Weight: 535.98

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Quality Control

Batch: Purity: 99.95%

99.95

Related Targets	HDAC JAK BET PKC PARP HIF PRMT EZH2 AMPK Histone Acetyltransferase
Other Histone Methyltransferase Inhibitors	Pinometostat (EPZ5676) 3-Deazaneplanocin A (DZNep) Hydrochloride BIX-01294 trihydrochloride EPZ004777 EPZ015666 (GSK3235025) UNC1999 EPZ005687 SGC 0946 MM-102 UNC0638

Solubility

In vitro
Batch:

DMSO : 99 mg/mL (184.7 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 66 mg/mL

Water : 4 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.950mg/ml (9.24mM)	Taking the 1 mL working solution as an example, add 50 μL of 99 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.820mg/ml (1.53mM)	Taking the 1 mL working solution as an example, add 50 μL of 16.4 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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.

Chemical Information, Storage & Stability

Molecular Weight	535.98	Formula	C₂₃H₂₅F₄N₃O₃S.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1627607-87-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			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

Mechanism of Action

Targets/IC₅₀/Ki	SETD7 (Cell-free assay) 0.33 nM(Ki) SETD7 (Cell-free assay) 2 nM
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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/25136132/

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