PFI-2

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase with IC50 value of 2.0 nM [1].
    SET domain containing (lysine methyltransferase) 7 (SETD7) is a protein lysine methyltransferase that acts as monomethyltransferase of lysine 4 on histone H3 (H3K4) and regulates DNA methyltransferase 1 (DNMT1) [1].
    PFI-2 is a potent and selective SETD7 methyltransferase inhibitor. (R)-PFI-2 inhibited human SETD7 methyltransferase activity with IC50 value of 2.0 nM. However, (S)-PFI-2 was 500-fold less active with IC50 value of only 1.0 µM. (R)-PFI-2 potently inhibited SETD7 with Morrison Kiapp value of 0.33 nM. (R)-PFI-2 occupied the peptide binding groove and effectively inhibited the binding of SETD7 substrates. In the presence of 20 μM SAM, (R)-PFI-2 bound to SETD7 with KD value of 4.2 nM in a SAM-dependent way. In HEK293 cells, (R)-PFI-2 (10 µM) bound to and stabilized SETD7. In Setd7+/+ murine embryonic fibroblasts (MEFs), (R)-PFI-2 increased nuclear localization of Yes-associated protein (YAP) and the expression of YAP target genes Ctgf, Gli2 and Cdc20 [1].
- Properties
  - Alternative Name
    
    8-fluoro-N-[(2R)-1-oxo-1-pyrrolidin-1-yl-3-[3-(trifluoromethyl)phenyl]propan-2-yl]-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide
    
    CAS Number
    
    1627676-59-8
    
    Molecular Formula
    
    C23H25F4N3O3S
    
    Molecular Weight
    
    499.52
    
    Appearance
    
    A solid
    
    Purity
    
    98.14%
    
    Solubility
    
    ≥50 mg/mL in DMSO; ≥1.51 mg/mL in H2O with gentle warming and ultrasonic; ≥8.12 mg/mL in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Chi Hin Wong, Chi Han Li, et al. "The Establishment of CDK9/ RNA PolII/H3K4me3/DNA Methylation Feedback Promotes HOTAIR Expression by RNA Elongation Enhancement in Cancer." bioRxiv. 2019 October 21.
    2. Li N, Yang L, et al. "BET bromodomain inhibitor JQ1 preferentially suppresses EBV-positive nasopharyngeal carcinoma cells partially through repressing c-Myc." Cell Death Dis. 2018 Jul 9;9(7):761. PMID:29988031

PFI-2

Background

We Also Recommend

K-Ras(G12C) inhibitor 12

LY2119620

URMC-099