Description
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: ≥12 months 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:
- http://www.thesgc.org/chemical-probes/epigenetics
Products are for research use only. Not for human use.
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