PFI-2

For research use only. Not for therapeutic Use.

  • CAT Number: I002101
  • CAS Number: 1627676-59-8
  • Molecular Formula: C₂₃H₂₅F₄N₃O₃S
  • Molecular Weight: 499.52
  • Purity: ≥95%
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PFI-2(Cat No.:I002101)is a small molecule inhibitor designed to target the protein Brd4, a member of the bromodomain and extra-terminal (BET) family. Brd4 plays a crucial role in regulating gene expression and is involved in the transcriptional activation of various genes, including those associated with cancer cell growth and survival. By inhibiting Brd4, PFI-2 is being investigated for its potential therapeutic effects in cancer, particularly in hematological malignancies and solid tumors. Preclinical studies have shown that PFI-2 can reduce tumor growth and increase sensitivity to other cancer therapies, though further clinical trials are needed.


Catalog Number I002101
CAS Number 1627676-59-8
Synonyms

8-fluoro-N-[(2R)-1-oxo-1-pyrrolidin-1-yl-3-[3-(trifluoromethyl)phenyl]propan-2-yl]-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide

Molecular Formula C₂₃H₂₅F₄N₃O₃S
Purity ≥95%
Target Histone Methyltransferase
Solubility 10 mM in DMSO
Storage Store at -20°C
IC50 2 nM
IUPAC 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
InChI InChI=1S/C23H25F4N3O3S/c24-20-13-18(12-16-6-7-28-14-19(16)20)34(32,33)29-21(22(31)30-8-1-2-9-30)11-15-4-3-5-17(10-15)23(25,26)27/h3-5,10,12-13,21,28-29H,1-2,6-9,11,14H2/t21-/m1/s1
InChIKey JCKGSPAAPQRPBW-OAQYLSRUSA-N
SMILES C1CCN(C1)C(=O)[C@@H](CC2=CC(=CC=C2)C(F)(F)F)NS(=O)(=O)C3=CC4=C(CNCC4)C(=C3)F
Reference

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<br>[1]. Barsyte-Lovejoy D, et al. (R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells. Proc Natl Acad Sci U S A. 2014 Sep 2;111(35):12853-8.

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