A potent

(R)-PFI-2 (hydrochloride) – 1 mg

Brand:
Cayman
CAS:
1627607-87-7
Storage:
-20
UN-No:
Non-Hazardous - /

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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Description

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

Formal name: 8-fluoro-1,2,3,4-tetrahydro-N-[(1R)-2-oxo-2-(1-pyrrolidinyl)-1-[[3-(trifluoromethyl)phenyl]methyl]ethyl]-6-isoquinolinesulfonamide, monohydrochloride

Synonyms:  (-)-PFI-2

Molecular weight: 536

CAS: 1627607-87-7

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Methyltransferases||Research Area|Epigenetics, Transcription, & Translation|Writers|Histone Methylation

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