PFI-2 (hydrochloride)
Synonym(s):(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
- CAS NO.:1627607-87-7
- Empirical Formula: C23H26ClF4N3O3S
- Molecular Weight: 535.98
- MDL number: MFCD28133380
- Update Date: 2024-10-28 16:48:35
What is PFI-2 (hydrochloride)?
Description
SET domain-
The Uses of PFI-2 (hydrochloride)
(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
storage
Store at -20°C
References
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
Properties of PFI-2 (hydrochloride)
Melting point: | >209°C (dec.) |
storage temp. | 2-8°C |
solubility | Soluble in DMSO (up to at least 25 mg/ml) |
form | powder |
color | white to beige |
Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months. |
Safety information for PFI-2 (hydrochloride)
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral |
Computed Descriptors for PFI-2 (hydrochloride)
New Products
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