PFI-2 hydrochloride
Based on 14 publication(s) in Google Scholar
PFI-2 ((R)-PFI-2 hydrochloride) hydrochloride is a potent and selective SET domain containing lysine methyltransferase 7 (SETD7) inhibitor. (R)-PFI-2 shows high inhibiting activity with IC50 value of 2.0 nM and (S)-PFI-2 shows inhibiting activity with IC50 value of 1.0 μM. PFI-2 hydrochloride can be used for the research of chronic kidney disease and inflammation response in the development of renal fibrosis.
For research use only. We do not sell to patients.
- Purity : 99.48%
- CAS No.: 1627607-87-7
- Formula: C23H26ClF4N3O3S
- Molecular Weight:535.98
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PFI-2 hydrochloride
More- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Sci Adv. 2023 May 26;9(21):eade4186. [Abstract]
- Acta Pharmacol Sin. 2022 Feb;43(2):457-469. [Abstract]
- Proc Natl Acad Sci U S A. 2019 Feb 19;116(8):2961-2966. [Abstract]
- Diabetes. 2025 Oct 1;74(10):1825-1838. [Abstract]
- Diabetes. 2025 Jun 1;74(6):969-982. [Abstract]
- Int J Mol Med. 2021 Dec;48(6):210. [Abstract]
- Biochem Pharmacol. 2024 Jan:219:115964. [Abstract]
- Med Oncol. 2023 Apr 12;40(5):146. [Abstract]
- Mol Carcinog. 2023 Aug;62(8):1119-1135. [Abstract]
- Biol Reprod. 2026 Jan 22:ioag005. [Abstract]
- Sci Total Environ. 2022 Dec 5;861:160682. [Abstract]
- Research Square Print. September 20th, 2022.
- Patent. US20180263995A1.
Customer Validation & Images
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RT-PCR
All Histone Methyltransferase Isoforms
More
Biological Activity
Description
IC50 & Target
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SETD7/KMT7 |
In Vitro
(R)-PFI-2 shows high inhibiting activity with IC50 value of 2.0 nM and (S)-PFI-2 shows inhibiting activity with IC50 value of 1.0 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
PFI-2 hydrochloride (i.p., 200 μM, twice a week) reduced ECM accumulation and fibroblasts activation after FA injury[2].
PFI-2 hydrochloride (i.p., 200 μM, twice a week) impeded Th2 cytokine signaling activation and M2 macrophage polarization[2].
PFI-2 hydrochloride (i.p., 200 μM, twice a week) suppressed M2 macrophages-myofibroblasts transition and myeloid myofibroblasts accumulation in the FA-treated kidneys[2].
PFI-2 hydrochloride (i.p., 200 μM, twice a week) attenuated macrophages M2 polarization and M2 macrophages-to-myofibroblasts transition in obstructed kidneys[2].
PFI-2 hydrochloride (i.p., 200 μM, twice a week) suppressed myeloid myofibroblast accumulation and renal fibrosis after UUO injury[2].
PFI-2 hydrochloride (i.p., 200 μM, twice a week) reduced the infiltration of inflammatory cells, the production of inflammatory molecules, and NF-κB activation in FA nephropathy[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice (8-10-week old, 20-25 g)[2]
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Dosage:200 μM (PFI-2 is diluted in 100 μL 0.1% (v/v) DMSO to a concentration of 200 μM/100 μL)
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Administration:intraperitoneal injection, twice a week
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Result:Presented less bone marrow-derived myofibroblasts, fewer CD206+/α-smooth muscle actin + cells and developed less renal fibrosis (P<0.01).
Reduced the infiltration of inflammatory cells and decreased the production of pro-inflammatory cytokines and chemokines in the kidneys after folic acid treatment (P<0.01).
Suppressed the accumulation of NF-κB p65+ cells in folic acid nephropathy (P<0.01).
Chemical Information
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CAS No. 1627607-87-7
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Appearance Solid
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Molecular Weight 535.98
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Formula C23H26ClF4N3O3S
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Color White to off-white
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SMILES
O=S(C1=CC2=C(CNCC2)C(F)=C1)(N[C@H](CC3=CC=CC(C(F)(F)F)=C3)C(N4CCCC4)=O)=O.[H]Cl
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Synonyms
(R)-PFI-2 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
Publications (14)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Sci Adv
PD-L1 methylation restricts PD-L1/PD-1 interactions to control cancer immune surveillance. [Abstract]2023 May 26;9(21):eade4186. PMID: 37235656 -
Acta Pharmacol Sin
2022 Feb;43(2):457-469. PMID: 33850273 -
Proc Natl Acad Sci U S A
2019 Feb 19;116(8):2961-2966. PMID: 30718431 -
Diabetes
Molecular Mechanisms of Human Pancreatic Islet Dysfunction Under Overnutrition Metabolic Stress. [Abstract]2025 Oct 1;74(10):1825-1838. PMID: 40773375 -
Diabetes
Targeting SETD7 Rescues Diabetes-induced Impairment of Angiogenic Response by Transcriptional Repression of Semaphorin 3G. [Abstract]2025 Jun 1;74(6):969-982. PMID: 40014026 -
Int J Mol Med
SETD7 regulates chondrocyte differentiation and glycolysis via the Hippo signaling pathway and HIF‑1α. [Abstract]2021 Dec;48(6):210. PMID: 34617577
PFI-2 hydrochloride purchased from MedChemExpress. Usage Cited in: Int J Mol Med. 2021 Dec;48(6):210. [Abstract]
mRNA expression levels of the key glycolysis enzymes GLUT1, LDHA, PGK1 and PKM2 of control and PFI-2 (10 μM) groups.
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Biochem Pharmacol
Activating transcriptional coactivator with PDZ-binding motif by (R)-PFI-2 attenuates osteoclastogenesis and prevents ovariectomized-induced osteoporosis. [Abstract]2024 Jan:219:115964. PMID: 38049011 -
Med Oncol
DDB1 regulates the activation-induced apoptosis of T cells via downregulating the expression of histone methyltransferase SETD7. [Abstract]2023 Apr 12;40(5):146. PMID: 37043057 -
Mol Carcinog
PRMT1 inhibition promotes ferroptosis sensitivity via ACSL1 upregulation in acute myeloid leukemia. [Abstract]2023 Aug;62(8):1119-1135. PMID: 37144835 -
Biol Reprod
SETD7 methylates the endometrial master regulator HOXA10 to facilitate H3K4me1 peaking for endometrial decidualization. [Abstract]2026 Jan 22:ioag005. PMID: 41568768 -
Sci Total Environ
2022 Dec 5;861:160682. PMID: 36481141 -
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Solvent & Solubility
In Vitro:
DMSO : ≥ 32 mg/mL (59.70 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 5.56 mg/mL (10.37 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.66 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.66 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 1 mg/mL (1.87 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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Fibrosis/Collagen Morphometry
Fibrosis and collagen morphometry is based on the quantitative visualization of fibrillar collagen deposition in tissue sections using histochemical stains such as Sirius Red (Picrosirius Red) or Masson's trichrome, followed by image-based or polarization-enhanced analysis to estimate collagen proportional area as a surrogate of extracellular matrix accumulation during fibrotic remodeling. Sirius Red combined with polarized light microscopy enhances detection of collagen fibers due to birefringence properties, enabling more specific visualization of collagen type I and III fibrils compared to conventional bright-field histology, while whole-section or region-restricted digital morphometry reduces field-selection bias in fibrosis assessment. Alternative quantitative approaches include second harmonic generation (SHG) and two-photon excited fluorescence microscopy, which enable label-free detection of fibrillar collagen and have been validated against histological staining and biochemica
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Collagen: Sirius Red Staining
Sirius Red or picrosirius red staining is a histochemical method for visualizing collagen-rich extracellular matrix in tissue sections, and collagen fibers are detected as red-stained structures under bright-field microscopy with enhanced birefringence under polarized light. Picrosirius red is useful for assessing total collagen organization, distribution, and fibrosis burden, but polarized color should not be interpreted as a definitive collagen type I versus type III readout because color is affected by fiber orientation, thickness, and packing.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
Masson’s Trichrome (collagen/trichrome staining) is a histological technique that differentially stains tissue compartments using sequential acidic dyes to distinguish collagen from muscle and cytoplasmic components based on dye affinity and tissue permeability differences, enabling visualization of fibrosis and connective tissue architecture in histological sections. The classical formulation typically uses Weigert's iron hematoxylin for nuclear staining, Biebrich scarlet-acid fuchsin for cytoplasm and muscle, and aniline blue (or light green variants) for collagen, producing a characteristic blue/green collagen signal contrasted against red cytoplasm and dark nuclei. The staining principle relies on selective displacement of smaller dye molecules by larger anionic dyes in collagen-rich regions under controlled acidified conditions, which enhances collagen-specific dye retention. This property makes the method widely used for fibrosis assessment in organs such as heart, liver, lung, a
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Purity & Documentation
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Data Sheet (283 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Yuzhen Niu, et al. Revealing inhibition difference between PFI-2 enantiomers against SETD7 by molecular dynamics simulations, binding free energy calculations and unbinding pathway analysis. Sci Rep. 2017 Apr 18;7:46547. [Content Brief]
[2]. Benquan Liu, et al. Pharmacological inhibition of SETD7 by PFI-2 attenuates renal fibrosis following folic acid and obstruction injury. Eur J Pharmacol. 2021 Jun 15;901:174097. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.8657 mL | 9.3287 mL | 18.6574 mL | 46.6435 mL |
| 5 mM | 0.3731 mL | 1.8657 mL | 3.7315 mL | 9.3287 mL | |
| 10 mM | 0.1866 mL | 0.9329 mL | 1.8657 mL | 4.6644 mL | |
| DMSO | 15 mM | 0.1244 mL | 0.6219 mL | 1.2438 mL | 3.1096 mL |
| 20 mM | 0.0933 mL | 0.4664 mL | 0.9329 mL | 2.3322 mL | |
| 25 mM | 0.0746 mL | 0.3731 mL | 0.7463 mL | 1.8657 mL | |
| 30 mM | 0.0622 mL | 0.3110 mL | 0.6219 mL | 1.5548 mL | |
| 40 mM | 0.0466 mL | 0.2332 mL | 0.4664 mL | 1.1661 mL | |
| 50 mM | 0.0373 mL | 0.1866 mL | 0.3731 mL | 0.9329 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
PFI-2 hydrochloride Related Classifications
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