PFI-2 HCl

Catalog No.S7294 Batch:S729404

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Technical Data

Formula

C23H25F4N3O3S.HCl
Molecular Weight 535.98 CAS No. 1627607-87-7
Solubility (25°C)* In vitro DMSO 99 mg/mL (184.7 mM)
Ethanol 99 mg/mL (184.7 mM)
Water 52 mg/mL (97.01 mM)
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.82mg/ml 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. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
4.95mg/ml 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. 
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 (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]

Protocol (from reference)

Selleck's PFI-2 HCl has been cited by 7 publications

Combined SET7/9 and CDK4 inhibition act synergistically against osteosarcoma [ Biochem Biophys Res Commun, 2024, 708:149808] PubMed: 38520914
H4K20me1 plays a dual role in transcriptional regulation of regeneration and axis patterning in Hydra [ Life Sci Alliance, 2023, 6(5)e202201619] PubMed: 36944423
BRD4770 functions as a novel ferroptosis inhibitor to protect against aortic dissection [ Pharmacol Res, 2022, 177:106122] PubMed: 35149187
Recapitulating early human development with 8C-like cells [ Cell Rep, 2022, 39(12):110994] PubMed: 35732112
SETD7 mediates spinal microgliosis and neuropathic pain in a rat model of peripheral nerve injury. [ Brain Behav Immun, 2019, 82:382-395] PubMed: 31505256
Epigenetic Reprogramming with Antisense Oligonucleotides Enhances the Effectiveness of Androgen Receptor Inhibition in Castration-Resistant Prostate Cancer [ Cancer Res, 2018, 78(20):5731-5740] PubMed: 30135193
[ Cell Death Dis, 2018, ] PubMed: 29988031

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.