PFI-2 (hydrochloride)
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- CAS-Nr.
- 1627607-87-7
- Englisch Name:
- PFI-2 (hydrochloride)
- Synonyma:
- (R)-PFI-2;PFI-2 HCl salt;PFI-2 (hydrochloride);(R)-PFI-2 (hydrochloride);PFI-2; PFI2;PFI 2;R PFI-2;R-PFI2;(1R)-1-[[3-(Trifluoromethyl)phenyl]methyl]-2-oxo-2-(1-pyrrolidinyl)ethyl]1,2,3,4-tetrahydro-6-isoquinolinesulfonamide hydrochloride;(R)-8-Fluoro-N-(1-oxo-1-(pyrrolidin-1-yl)-3-(3-(trifluoromethyl)phenyl)propan-2-yl)-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide hydrochloride;macrophage,chronic kidney disease,inhibit,Histone Methyltransferase,PFI-2,Inhibitor,SET domain containing lysine methyltransferase 7 (SETD7),PFI2 hydrochloride,renal fibrosis,inflammation,PFI 2,PFI2,PFI 2 hydrochloride
- CBNumber:
- CB83041444
- Summenformel:
- C23H26ClF4N3O3S
- Molgewicht:
- 535.98
- MOL-Datei:
- 1627607-87-7.mol
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PFI-2 (hydrochloride) Eigenschaften
- Schmelzpunkt:
- >209°C (dec.)
- storage temp.
- 2-8°C
- L?slichkeit
- Soluble in DMSO (up to at least 25 mg/ml)
- Aggregatzustand
- powder
- Farbe
- white to beige
- Stabilit?t:
- Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
Bildanzeige (GHS) |
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Alarmwort |
Warnung |
Gefahrenhinweise |
Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
H302 |
Gesundheitssch?dlich bei Verschlucken. |
Akute Toxizit?t oral |
Kategorie 4 |
Warnung |
src="/GHS07.jpg" width="20" height="20" /> |
P264, P270, P301+P312, P330, P501 |
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Sicherheit |
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PFI-2 (hydrochloride) Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
SET domain-
containing protein 7/9 (SET7/9) is a histone methyltransferase that monomethylates lysine 4 of histone H3, which generates a specific tag for epigenetic transcriptional activation. It plays a role in the transcriptional activation of tumor suppressor p53 in response to DNA damage as well as the transcription factor TAF10. (R)-PFI-2 is a potent, cell-permeable inhibitor of SET7/9 (IC
50 = 2 nM) that demonstrates greater than 1,000-fold selectivity over a panel of 18 other methyltransferases. Its enantiomer, (S)-PFI-2 , is 500-fold less active (IC
50 = 1 μM). See the
Structural Genomics Consortium (SGC) website for more information.
Verwenden
(1R)-1-[[3-(Trifluoromethyl)phenyl]methyl]-2-oxo-2-(1-pyrrolidinyl)ethyl]1,2,3,4-tetrahydro-6-isoquinolinesulfonamide Hydrochloride known as (-)-PFI-2 HCl is a cell permeable inhibitor of SET Domain-Containing protein 7/9 (SET 7/9) which plays a role in tumorigenesis in cell cancer lines.
Biochem/physiol Actions
(R)-PFI-2 is a histone-lysine N-methyltransferase (HKMT) inhibitor selective for SETD7 (also known as SET9). (R)-PFI-2 has an IC50 value of 2 nM and 1000-fold selectivity over other methyltransferases and other non-epigenetic targets. For full characterization details, please visit the PFI-2 probe summary on the Structural Genomics Consortium (SGC) website.(S)-PFI-2, an enantiomer of (R)-PFI-2, is used as a negative control. (S)-PFI-2 is available from Sigma. To learn more about and purchase (S)-PFI-2, click here.To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
PFI-2 (hydrochloride) Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
PFI-2 (hydrochloride) Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 71)Lieferanten
- PFI-2 (hydrochloride)
- PFI-2 HCl salt
- (R)-PFI-2 (hydrochloride)
- (R)-PFI-2
- PFI-2; PFI2;PFI 2;R PFI-2;R-PFI2
- (1R)-1-[[3-(Trifluoromethyl)phenyl]methyl]-2-oxo-2-(1-pyrrolidinyl)ethyl]1,2,3,4-tetrahydro-6-isoquinolinesulfonamide hydrochloride
- (R)-8-Fluoro-N-(1-oxo-1-(pyrrolidin-1-yl)-3-(3-(trifluoromethyl)phenyl)propan-2-yl)-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide hydrochloride
- macrophage,chronic kidney disease,inhibit,Histone Methyltransferase,PFI-2,Inhibitor,SET domain containing lysine methyltransferase 7 (SETD7),PFI2 hydrochloride,renal fibrosis,inflammation,PFI 2,PFI2,PFI 2 hydrochloride
- 1627607-87-7
- C23H25F4N3O3SHCl
- C23H26ClF4N3O3S
- API