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How to Cite 1. For In-Text Citation (Materials & Methods): 2. For Key Resources Table: |
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Technical Data
| Formula | C23H25F4N3O3S.HCl |
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| Molecular Weight | 535.98 | CAS No. | 1627607-87-7 | ||||
| Solubility (25°C)* | In vitro | DMSO | 99 mg/mL (184.7 mM) | ||||
| Ethanol | 25 mg/mL (46.64 mM) | ||||||
| Water | 7 mg/mL (13.06 mM) | ||||||
| In vivo (Add solvents to the product individually and in order) |
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* <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.) |
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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. | ||||
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| Targets |
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| 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. |
Protocol (from reference)
References
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Selleck's PFI-2 HCl Has Been Cited by 12 Publications
| BRD4770 functions as a novel ferroptosis inhibitor to protect against aortic dissection [ Pharmacological Research, March 2022, 106122] | PubMed: 35149187 |
| Microglial epigenetic memory is associated with accelerated resolution of inflammatory pain induced by prophylactic macrophage-derived small extracellular vesicles [ bioRxiv, January 16, 2026, 2026.01.15.699551] | PubMed: 41648229 |
| Microglial epigenetic memory is associated with accelerated resolution of inflammatory pain induced by prophylactic macrophage-derived small extracellular vesicles [ bioRxiv, 2026, nan] | PubMed: 41648229 |
| SETD7 is a novel therapeutic target for multiple myeloma with t(11;14)+ [ Research Square, 2025, nan] | |
| 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 |
| Inhibition of cGAS-STING by JQ1 alleviates oxidative stress-induced retina inflammation and degeneration [ Cell Death & Differentiation, 2022, 1816-1833] | PubMed: 35347235 |
| 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 |
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