GNE-272

  • Chemical Properties
CAS No. 1936428-93-1 Cat. No. BCP19967
Name GNE-272
Synonyms GNE272;GNE 272;
Formula C22H25FN6O2 M. Wt 424.48
  • Biological Activity
Description GNE-272 is a potent and selective in Vivo Probe for the Bromodomains of CBP/EP300 (CBP IC50 = 0.02 μM, EP300 IC50 = 0.03 μM, BRET IC50 = 0.41 μM, BRD4(1) C50 = 13 μM).GNE-272 showed a marked antiproliferative effect in hematologic cancer cell lines and modulates MYC expression in vivo that corresponds with antitumor activity in an AML tumor model. CBP has also been implicated in neurological disorders where a CBP bromodomain inhibitor has been shown to reduce expression of a regulator of G-protein signaling (RGS4).
Pathways Epigenetics 
Targets Histone Acetyltransferase Epigenetic Reader Domain 

Structure

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