PFI-2

• 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].

• Product Name Alternative :

  (R) -PFI-2

• UNSPSC :

  12352005

• Hazard Statement :

  H302, H315, H319, H335

• Target :

  Histone Methyltransferase

• Type :

  Reference compound

• Related Pathways :

  Epigenetics

• Applications :

  Cancer-programmed cell death

• Field of Research :

  Cancer; Infection; Inflammation/Immunology

• Assay Protocol :

  https://www.medchemexpress.com/PFI-2.html

• Purity :

  99.68

• Solubility :

  DMSO : ≥ 100 mg/mL

• 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

• Molecular Formula :

  C23H25F4N3O3S

• Molecular Weight :

  499.52

• Precautions :

  H302, H315, H319, H335

• References & Citations :

  [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.|[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.

• Shipping Conditions :

  Blue Ice

• Storage Conditions :

  -20°C (Powder, sealed storage, away from moisture)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  SETD7/KMT7

• Citation 01 :

  Acta Pharmacol Sin. 2022 Feb;43 (2) :457-469.|Biochem Pharmacol. 2024 Jan:219:115964.|Med Oncol. 2023 Apr 12;40 (5) :146.|Patent. US20180263995A1.|Sci Adv. 2023 May 26;9 (21) :eade4186.|Sci Total Environ. 2022 Dec 5;861:160682.|Diabetes. 2025 Jun 1;74 (6) :969-982.|Diabetes. 2025 Oct 1;74 (10) :1825-1838.|Int J Mol Med. 2021 Dec;48 (6) :210.|Mol Carcinog. 2023 Aug;62 (8) :1119-1135.|Proc Natl Acad Sci U S A. 2019 Feb 19;116 (8) :2961-2966. |Research Square Print. September 20th, 2022.

• CAS Number :

  [1627676-59-8]