PFI-2
Based on 14 publication(s) in Google Scholar
PFI-2 ((R)-PFI-2 hydrochloride) hydrochloride, a chemical probe, 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: 99.68%
- CAS No.: 1627676-59-8
- Formula: C23H25F4N3O3S
- Molecular Weight:499.52
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (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
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PFI-2
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.
All Histone Methyltransferase Isoforms
More
Biological Activity
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SETD7/KMT7 |
(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.
PFI-2 (i.p., 200 μM, twice a week) reduced ECM accumulation and fibroblasts activation after FA injury[2].
PFI-2 (i.p., 200 μM, twice a week) impeded Th2 cytokine signaling activation and M2 macrophage polarization[2].
PFI-2 (i.p., 200 μM, twice a week) suppressed M2 macrophages-myofibroblasts transition and myeloid myofibroblasts accumulation in the FA-treated kidneys[2].
PFI-2 (i.p., 200 μM, twice a week) attenuated macrophages M2 polarization and M2 macrophages-to-myofibroblasts transition in obstructed kidneys[2].
PFI-2 (i.p., 200 μM, twice a week) suppressed myeloid myofibroblast accumulation and renal fibrosis after UUO injury[2].
PFI-2 (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.
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. 1627676-59-8
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Appearance Solid
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Molecular Weight 499.52
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Formula C23H25F4N3O3S
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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
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Synonyms
(R)-PFI-2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (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 -
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
DMSO : ≥ 100 mg/mL (200.19 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (279 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0019 mL | 10.0096 mL | 20.0192 mL | 50.0480 mL |
| 5 mM | 0.4004 mL | 2.0019 mL | 4.0038 mL | 10.0096 mL | |
| 10 mM | 0.2002 mL | 1.0010 mL | 2.0019 mL | 5.0048 mL | |
| 15 mM | 0.1335 mL | 0.6673 mL | 1.3346 mL | 3.3365 mL | |
| 20 mM | 0.1001 mL | 0.5005 mL | 1.0010 mL | 2.5024 mL | |
| 25 mM | 0.0801 mL | 0.4004 mL | 0.8008 mL | 2.0019 mL | |
| 30 mM | 0.0667 mL | 0.3337 mL | 0.6673 mL | 1.6683 mL | |
| 40 mM | 0.0500 mL | 0.2502 mL | 0.5005 mL | 1.2512 mL | |
| 50 mM | 0.0400 mL | 0.2002 mL | 0.4004 mL | 1.0010 mL | |
| 60 mM | 0.0334 mL | 0.1668 mL | 0.3337 mL | 0.8341 mL | |
| 80 mM | 0.0250 mL | 0.1251 mL | 0.2502 mL | 0.6256 mL | |
| 100 mM | 0.0200 mL | 0.1001 mL | 0.2002 mL | 0.5005 mL |
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