Basic information Safety Supplier Related

PFI-2 (hydrochloride)

Basic information Safety Supplier Related

PFI-2 (hydrochloride) Basic information

Product Name:
PFI-2 (hydrochloride)
Synonyms:
  • 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
CAS:
1627607-87-7
MF:
C23H26ClF4N3O3S
MW:
535.98
Product Categories:
  • API
Mol File:
1627607-87-7.mol
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PFI-2 (hydrochloride) Chemical Properties

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.
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PFI-2 (hydrochloride) Usage And Synthesis

Description

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.

Uses

(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

PFI-2 (hydrochloride)Supplier

Shanghai Dongyang Biotechnology Co., Ltd. Gold
Tel
0512-0512-13601744364 13601744364
Email
chemsharker@126.com
Jiangsu Aikon Biopharmaceutical R&D co.,Ltd.
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025-66099280 17798518460
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cfzhang@aikonchem.com
Haoyuan Chemexpress Co., Ltd.
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021-58950125
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info@chemexpress.com
MedChemexpress LLC
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021-58955995
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sales@medchemexpress.cn
Sigma-Aldrich
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021-61415566 800-8193336
Email
orderCN@merckgroup.com