2. Epigenetics
  3. Histone Methyltransferase
  4. PFI-2

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.

PFI-2

PFI-2 Chemical Structure

CAS No. : 1627676-59-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 14 publication(s) in Google Scholar

Other Forms of PFI-2:

PFI-2 Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2].

IC50 & Target

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.

PFI-2 Related Antibodies
In Vivo

PFI-2 (i.p., 200 μM, twice a week) attenuates the progression of renal fibrosis and preserves renal function in FA nephropathy[2].
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.

Animal Model: Male C57BL/6 mice (8-10 week old, 20-25 g)[2]
Dosage: 200 μM (PFI-2 is diluted in 100 μL 0.1% (v/v) DMSO to a concentration of 200 μM/100 μL)
Administration: intraperitoneal injection, twice a week
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).
Molecular Weight

499.52

Formula

C23H25F4N3O3S
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0019 mL 10.0096 mL 20.0192 mL
5 mM 0.4004 mL 2.0019 mL 4.0038 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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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PFI-2 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PFI-21627676-59-8(R)-PFI-2PFI2PFI 2Histone MethyltransferaseSET domain containing lysine methyltransferase 7 (SETD7)renal fibrosisinflammationmacrophagechronic kidney diseaseInhibitorinhibitorinhibit

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