PFI-2, SETD7 Histone Lysine Methyltransferase Inhibitor

PFI-2 is a novel potent and selective SETD7 histone lysine methyltransferase inhibitor with 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=18nM), and biotinylated PFI-2 interacts with SETD7 in pull-down studies.

Product information

CAS Number: 1627676-59-8

Molecular Weight: 499.52

Formula: C23H25F4N3O3S

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

Smiles: O=C([C@@H](CC1C=C(C=CC=1)C(F)(F)F)NS(=O)(=O)C1=CC(F)=C2CNCCC2=C1)N1CCCC1

InChiKey: JCKGSPAAPQRPBW-OAQYLSRUSA-N

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

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

PFI-2 was used at 1 µM in vitro.

References:

1. http://www.thesgc.org/chemical-probes/epigenetics

Products are for research use only. Not for human use.