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[1][2].

Product Specifications

CAS Number

[1627676-59-8]

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.