PFI-<wbr/>1

PFI-1

CAT N°: 11155
Price:

From 57.00 48.45

Bromodomains recognize acetylated lysine residues and recruit regulatory complexes to acetylated nucleosomes, thereby controlling chromatin structure and gene expression. The isolated individual or tandem bromodomains of bromodomain-containing protein (BRD) 2 and BRD4 bind acetylated histone tails, which couples histone acetylation marks to the transcriptional regulation of target promoters. Small molecule inhibitors of bromodomain interactions hold promise as useful therapeutics for human disease.{19044,19929,19950} PFI-1 is a BET bromodomain inhibitor that exhibits inhibitory activity at BRD2 and BRD4. In an AlphaScreen assay it has been shown to inhibit BRD2 bromodomain 2 and BRD4 bromodomain 1 with IC50 values of 98 nM and 0.22 ?M, respectively. See the Structural Genomics Consortium (SGC) website for more information.

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 2-methoxy-N-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide
  • Correlated keywords
    • BETs bromodomains inhibits inhibitors inhibition acetylateds lysines residues regulations nucleosomes chromatins structures genes expressions tandem bromodomain-containing proteins BRDs BRD2 BRD4 histones tails acetylations transcriptional targets promoters molecules therapeutics humans diseases inhibitory AlphaScreens assays PFI-1 PFI1 PFI 1 2 4 PF06405761 PFs 06405761 6405761 PF-06405761
  • Product Overview:
    Bromodomains recognize acetylated lysine residues and recruit regulatory complexes to acetylated nucleosomes, thereby controlling chromatin structure and gene expression. The isolated individual or tandem bromodomains of bromodomain-containing protein (BRD) 2 and BRD4 bind acetylated histone tails, which couples histone acetylation marks to the transcriptional regulation of target promoters. Small molecule inhibitors of bromodomain interactions hold promise as useful therapeutics for human disease.{19044,19929,19950} PFI-1 is a BET bromodomain inhibitor that exhibits inhibitory activity at BRD2 and BRD4. In an AlphaScreen assay it has been shown to inhibit BRD2 bromodomain 2 and BRD4 bromodomain 1 with IC50 values of 98 nM and 0.22 ?M, respectively. See the Structural Genomics Consortium (SGC) website for more information.

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