PFI-2
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- CAS-Nr.
- 1627676-59-8
- Englisch Name:
- PFI-2
- Synonyma:
- PFI-2;CS-1808;PFI-2 HCl;R-PFI-2 HCl;PFI-2 USP/EP/BP;8-fluoro-1,2,3,4-tetrahydro-N-[(1R)-2-oxo-2-(1-pyrrolidinyl)-1-[[3-(trifluoromethyl)phenyl]methyl]ethyl]-6-isoquinolinesulfonamide;6-Isoquinolinesulfonamide, 8-fluoro-1,2,3,4-tetrahydro-N-[(1R)-2-oxo-2-(1-pyrrolidinyl)-1-[[3-(trifluoromethyl)phenyl]methyl]ethyl]-;(R)-8-fluoro-N-(1-oxo-1-(pyrrolidin-1-yl)-3-(3-(trifluoromethyl)phenyl)propan-2-yl)-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide (R)-PFI 2 hydrochloride
- CBNumber:
- CB62729655
- Summenformel:
- C23H25F4N3O3S
- Molgewicht:
- 499.52
- MOL-Datei:
- 1627676-59-8.mol
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PFI-2 Eigenschaften
- Siedepunkt:
- 642.7±65.0 °C(Predicted)
- Dichte
- 1.371±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- Löslichkeit
- ≥50 mg/mL in DMSO; ≥1.51 mg/mL in H2O with gentle warming and ultrasonic; ≥8.12 mg/mL in EtOH
- Aggregatzustand
- solid
- pka
- 8.95±0.20(Predicted)
Sicherheit
- Risiko- und Sicherheitserklärung
- Gefahreninformationscode (GHS)
PFI-2 Chemische Eigenschaften,Einsatz,Produktion Methoden
Verwenden
PFI-2 is a potent and selective lysine methyltransferase SETD7 inhibitor which is a crucial factor in many disease related pathways.
Enzyminhibitor
This SETD7 inhibitor (FW = 499.52 g/mol; CAS 1627676-59-8; IUPAC: 8- fluoro-1,2,3,4-tetrahydro-N-[(1R)-2-oxo-2-(1-pyrrolidinyl)-1-[[3- (trifluoromethyl)phenyl]methyl]ethyl]-6-isoquinolinesulfonamide, targets the SET domain containing lysine methyltransferase, or SETD7 (Ki = 0.33 nM; IC50 = 2 nM), showing 1000-times selectivity versus other methyltransferases and other non-epigenetic targets. (R)-PFI-2 exhibits an unusual cofactor-dependent and substrate-competitive inhibitory mechanism by occupying the substrate peptide binding groove of SETD7, including the catalytic lysine-binding channel, and by making direct contact with the donor methyl group of the cofactor, S-adenosylmethionine. In murine embryonic fibroblasts, (R)-PFI-2 treatment phenocopies the effects of Setd7 deficiency on Hippo pathway signaling, via modulation of the transcriptional coactivator Yes-associated protein (YAP) and regulation of YAP target genes. In confluent MCF7 cells, (R)-PFI-2 rapidly alters YAP localization, suggesting continuous and dynamic regulation of YAP by the methyltransferase activity of SETD7.
PFI-2 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
PFI-2 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.
Global( 48)Lieferanten
- (R)-8-fluoro-N-(1-oxo-1-(pyrrolidin-1-yl)-3-(3-(trifluoromethyl)phenyl)propan-2-yl)-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide (R)-PFI 2 hydrochloride
- PFI-2 HCl
- 8-fluoro-1,2,3,4-tetrahydro-N-[(1R)-2-oxo-2-(1-pyrrolidinyl)-1-[[3-(trifluoromethyl)phenyl]methyl]ethyl]-6-isoquinolinesulfonamide
- PFI-2
- R-PFI-2 HCl
- CS-1808
- 6-Isoquinolinesulfonamide, 8-fluoro-1,2,3,4-tetrahydro-N-[(1R)-2-oxo-2-(1-pyrrolidinyl)-1-[[3-(trifluoromethyl)phenyl]methyl]ethyl]-
- PFI-2 USP/EP/BP
- 1627676-59-8
- C23H25F4N3O3S
- Inhibitors
