PFI-2 (hydrochloride)

• UNSPSC Description:

  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[1][2].

• Target Antigen:

  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-hydrochloride.html

• Purity:

  99.52

• Solubility:

  DMSO : ≥ 32 mg/mL|H2O : 5.56 mg/mL (ultrasonic)

• 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

• Molecular Weight:

  535.98

• 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.Int J Mol Med. 2021 Dec;48(6):210.|Mol Carcinog. 2023 May 5.|Proc Natl Acad Sci U S A. 2019 Feb 19;116(8):2961-2966. |Research Square Print. September 20th, 2022.|Acta Pharmacol Sin. 2021 Apr 13.|Biochem Pharmacol. 2023 Dec 2:115964.|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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  4°C (Powder, sealed storage, away from moisture)

• Clinical Information:

  No Development Reported

• CAS Number:

  1627607-87-7