MW 499.5 Da, Purity >98%. A potent and selective SETD7 histone lysine methyltransferase inhibitor. Ki = 0.33 nM and IC50 = 2 nM against SETD7. It displays > 1000-fold selectivity against DNMT1 and many other methyltransferases. No activity against 134 ion channel, GPCR, and enzyme targets (<35% inhibition at 10 μM). PFI-2 potently inhibits SETD7 in MCF7 cells.
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Publications
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- Scientific reports 7:465472017Revealing inhibition difference between PFI-2 enantiomers against SETD7 by molecular dynamics simulations, binding free energy calculations and unbinding pathway analysis.Applications:Unspecified applicationReactive species:Unspecified reactive speciesYuzhen Niu et. al.PubMed 28417976
- Analytical and bioanalytical chemistry 409:3767-37772017A direct label-free MALDI-TOF mass spectrometry based assay for the characterization of inhibitors of protein lysine methyltransferases.Applications:Unspecified applicationReactive species:Unspecified reactive speciesKarine Guitot et. al.PubMed 28389916
- Journal of medicinal chemistry 58:1596-6292014Selective inhibitors of protein methyltransferases.Applications:Unspecified applicationReactive species:Unspecified reactive speciesH Ümit Kaniskan,Kyle D Konze,Jian JinPubMed 25406853
- Proceedings of the National Academy of Sciences of 111:12853-82014(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells.Applications:Unspecified applicationReactive species:Unspecified reactive speciesDalia Barsyte-Lovejoy et. al.PubMed 25136132
Key facts
- CAS number
- 1627676-59-8
- Purity
- > 98%
- Form
- Solid
- Molecular weight
- 499.5 Da
- Molecular formula
- C23H25F4N3O3S
- PubChem identifier
- 71300326
- Nature
- Synthetic
Target data
Alternative names
FLJ21193, H3 K4 HMTase, H3-K4-HMTase SETD7, H4 lysine 4 specific, Histone H3 K4 methyltransferase, Histone H3 lysine 4 specific methyltransferase, Histone H3-K4 methyltransferase SETD7, Histone H4 K4 methyltransferase, Histone lysine N methyltransferase H3 lysine 4 specific SET7, Histone-lysine N-methyltransferase, Histone-lysine N-methyltransferase SETD7, KIAA1717, KMT7, Lysine N-methyltransferase 7, Lysine methyltransferase, OTTHUMP00000164543, OTTHUMP00000220049, SET 7/9, SET 9, SET domain containing (lysine methyltransferase) 7, SET domain-containing protein 7, SET domain-containing protein 8, SETD7_HUMAN
Recommended products
MW 499.5 Da, Purity >98%. A potent and selective SETD7 histone lysine methyltransferase inhibitor. Ki = 0.33 nM and IC50 = 2 nM against SETD7. It displays > 1000-fold selectivity against DNMT1 and many other methyltransferases. No activity against 134 ion channel, GPCR, and enzyme targets (<35% inhibition at 10 μM). PFI-2 potently inhibits SETD7 in MCF7 cells.
Key facts
- CAS number
- 1627676-59-8
- Purity
- > 98%
- Form
- Solid
- Molecular weight
- 499.5 Da
- Molecular formula
- C23H25F4N3O3S
- PubChem identifier
- 71300326
- Nature
- Synthetic
- Biochemical 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
- Biological description
A potent and selective SETD7 histone lysine methyltransferase inhibitor. Ki = 0.33 nM and IC50 = 2 nM against SETD7. It displays > 1000-fold selectivity against DNMT1 and many other methyltransferases. No activity against 134 ion channel, GPCR, and enzyme targets (<35% inhibition at 10 μM). PFI-2 potently inhibits SETD7 in MCF7 cells.
- Canonical SMILES
- C1CCN(C1)C(=O)C(CC2=CC(=CC=C2)C(F)(F)F)NS(=O)(=O)C3=CC4=C(CNCC4)C(=C3)F
- Isomeric 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
- 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
- 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
Storage
- Shipped at conditions
- Blue Ice
- Appropriate short-term storage conditions
- -20°C
- Appropriate long-term storage conditions
- -20°C
- Storage information
- Store in the dark
Notes
This product is manufactured by BioVision, an Abcam company and was previously called B1259 PFI-2. B1259-25 is the same size as the 25 mg size of ab223601.
Protect from air.
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1 product image
Chemical Structure - PFI-2, SETD7 histone lysine methyltransferase inhibitor (ab223601)
2D chemical structure image of ab223601, PFI-2, SETD7 histone lysine methyltransferase inhibitor
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