BIX01294 hydrochloride

  • Chemical Properties
CAS No. 1392399-03-9 Cat. No. BCP14567
Name BIX01294 hydrochloride
Synonyms BIX-01294 hydrochloride;BIX 01294 hydrochloride;
Formula C28H38N6O2•3HCl M. Wt 600.02
  • Biological Activity
Description BIX-01294 specifically inhibited G9a (H3K9me2) and, to a lesser extent, the closely related GLP enzyme (primarily H3K9me3), with an IC50 of 1.7 μM for G9a and 38 μM for GLP. BIX-01294 inhibits G9a in an uncompetitive manner with SAM. BIX-01294 (4.1μM) reduces H3K9me2 Levels in Bulk Histone Preparations from wt ES cells, mouse embryonic fibroblasts and HeLa cells, but not in G9a deficient stem cells. BIX-01294 is a valuable inhibitor for the transient modulation of chromosomal H3K9me2. BIX-01294 Reduces H3K9me2 at Several G9a Target Genes including Bim1 and Serac1. BIX01294 could reactivate expression of HIV-1 from latently infected cells such as ACH-2 and OM10.1.
Pathways Epigenetics 
Targets Histone Methyltransferase 

Structure

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