2. Cytoskeleton Cell Cycle/DNA Damage Apoptosis
  3. Microtubule/Tubulin Apoptosis
  4. 1627676-59-8

1627676-59-8

PFI-2 Chemical Structure

1627676-59-8

Chemical Structure

  • PFI-2
  • Synonym(s): (R)-PFI-2
  • CAS No: 1627676-59-8
    Formula: C23H25F4N3O3S
    Molecular Weight: 499.52
  • IUPAC Name: (R)-8-fluoro-N-(1-oxo-1-(pyrrolidin-1-yl)-3-(3-(trifluoromethyl)phenyl)propan-2-yl)-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide
  • InChIKey: JCKGSPAAPQRPBW-OAQYLSRUSA-N
  • 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

Biological Activity: 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].

Cat. No. Product Name Purity Description
HY-18627 PFI-2 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.

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]

Keywords:

PFI-2