PFI-2 | B1259

PFI-2 is a novel potent and selective SETD7 histone lysine methyltransferase inhibitor (IC₅₀ ~2 nM). It has > 100-fold selectivity over other methyltransferases and other non-epigenetic targets. PFI-2 has been shown to bind to SETD7 by ITC (Kd = 18 nM), and biotinylated PFI-2 interacts with SETD7 in pull-down studies.

PFI-2 is a novel potent and selective SETD7 histone lysine methyltransferase inhibitor (IC₅₀ ~2 nM). It has > 100-fold selectivity over other methyltransferases and other non-epigenetic targets. PFI-2 has been shown to bind to SETD7 by ITC (Kd = 18 nM), and biotinylated PFI-2 interacts with SETD7 in pull-down studies.

B1259 | PFI-2 DataSheet

Alternate Name/Synonyms: (R)-8-fluoro-N-(1-oxo-1-(pyrrolidin-1-yl)-3-(3-(trifluoromethyl)phenyl)propan-2-yl)-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide

Appearance: Crystaline solid

Formulation: N/A

CAS Number: 1627676-59-8

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₂₃H₂₅F₄N₃O₃S

Molecular Weight: 499.52

Cell-Permeable?: Yes

Purity: ≥98% by HPLC

Solubilities: DMSO (>30 mg/ml)

Handling: Protect from air and light

Country of Origin: USA

Tag Line: A potent and selective SETD7 histone lysine methyltransferase inhibitor

MDL Number: N/A

PubChem CID: 71300326

SMILES: C1CCN(C1)C(=O)C(CC2=CC(=CC=C2)C(F)(F)F)NS(=O)(=O)C3=CC(=C4CNCCC4=C3)F

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

InChi Key: JCKGSPAAPQRPBW-OAQYLSRUSA-N