PFI-2 HCl (R-)

SKU: orb1302737

Description

PFI-2 hydrochloride is a potent and selective cell-active inhibitor of the SETD7 methyltransferase, exhibiting an IC50 of 2 nM. It is the (R)-enantiomer, showing 500-fold greater activity than its (S)-counterpart. This compound is a valuable chemical probe for studying lysine methylation in epigenetic regulation, cancer biology, and inflammation research in cellular and biochemical assays.

Research Area

Epigenetics & Chromatin, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1627607-87-7
• MW: 535.98
• Purity: >98%
• Formula: C₂₃H₂₅F₄N₃O₃S HCl
• SMILES: Cl.Fc1cc(cc2CCNCc12)S(=O)(=O)N[C@H](Cc1cccc(c1)C(F)(F)F)C(=O)N1CCCC1
• Target: Protein methyltransferase
• Solubility: Soluble in DMSO (up to at least 25 mg/ml)

Bioactivity

• Target IC50:
  SETD7:2 nM
• In Vitro:
  (R)-PFI-2 is highly selective (>1,000-fold) for SETD7, over a panel of 18 other human protein methyltransferases and DNMT1, and was shown to be inactive against 134 additional ion channel, GPCR, and enzyme targets (<35% inhibition at 10 μM). (R)-PFI-2 binds to SETD7 only in the presence of SAM. PFI-766, a biotinylated variant of (R)-PFI-2 that retains the ability to bind and inhibit SETD7 (IC50 110 ± 26 nM in our in vitro enzymatic assay).
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

renal fibrosis, SETD7, SET domain containing lysine methyltransferase 7 (SETD7), PFI 2, PFI 2 Hydrochloride, PFI 2 hydrochloride, PFI2, PFI-2, PFI-2 HCl, PFI2 hydrochloride, PFI2 Hydrochloride, PFI-2 Hydrochloride, chronic kidney disease, (R)-PFI-2 hydrochloride, inflammation, inhibit, macrophage, Histone Methyltransferase, HistoneMethyltransferase, Inhibitor

Compound Identifiers

PubChem CID

78243738