PFI-2 (hydrochloride) Struktur

PFI-2 (hydrochloride)

Bezeichnung:PFI-2 (hydrochloride)

CAS-Nr1627607-87-7

Englisch Name:PFI-2 (hydrochloride)

CBNumberCB83041444

SummenformelC23H26ClF4N3O3S

Molgewicht535.98

MOL-Datei1627607-87-7.mol

PFI-2 (hydrochloride) physikalisch-chemischer Eigenschaften

Schmelzpunkt	>209°C (dec.)
storage temp.	2-8°C
Löslichkeit	Soluble in DMSO (up to at least 25 mg/ml)
Aggregatzustand	powder
Farbe	white to beige
Stabilität	Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.

Gefahreninformationscode (GHS)

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 (IC₅₀ = 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 (IC₅₀ = 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
Lager
Store at -20°C
Einzelnachweise
1)?Barsyte-Lovejoy?et al.?(2014),?(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells;?Proc. Natl. Acad. Sci. USA?111?12853

PFI-2 (hydrochloride) Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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