(R)-<wbr/>PFI-<wbr/>2 (hydro<wbr>chloride)

(R)-PFI-2 (hydrochloride)

CAT N°: 14678
Price:

From 85.00 72.25

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.{16846,17223} (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.{26909} Its enantiomer, (S)-PFI-2 (Item No. 18119), is 500-fold less active (IC50 = 1 µM).{26909} See the Structural Genomics Consortium (SGC) website for more information.

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 8-fluoro-1,2,3,4-tetrahydro-N-[(1R)-2-oxo-2-(1-pyrrolidinyl)-1-[[3-(trifluoromethyl)phenyl]methyl]ethyl]-6-isoquinolinesulfonamide, monohydrochloride
  • Correlated keywords
    • epigenetic methyltransferase inhibitor cancer SET7/9 SETD7 transcription inhibit cell-permeable SET domain-containing lysine 7 protein 7/9 histone transcriptional activation tumor suppressor p53 DNA damage deoxyribonucleic acid factor TAF10 TAF 10 PFI2 Structural Genomic Consortium SGC
  • Product Overview:
    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.{16846,17223} (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.{26909} Its enantiomer, (S)-PFI-2 (Item No. 18119), is 500-fold less active (IC50 = 1 µM).{26909} See the Structural Genomics Consortium (SGC) website for more information.

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