Catalog Number: 3364
Chemical Name: 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine trihydrochloride
Biological Activity
GLP and G9a histone lysine methyltransferase inhibitor (IC50 values are 0.7 and 1.7 μM respectively) that displays no activity at other histone methyltransferases up to 37 μM. Modulates H3K9me2 levels in mammalian cells and potentiates induction of pluripotent stem cells from somatic cells in vitro.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in water and to 100 mM in DMSO
  • Purity:
  • Storage:
    Desiccate at RT
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294.
    Chang et al.
    Nat.Struct.Mol.Biol., 2009;16:312
  2. Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase.
    Kubicek et al.
    Mol.Cell, 2007;25:473
  3. Induction of pluripotent stem cells from mouse embryonic fibroblasts by Oct4 and Klf4 with small-molecule compounds.
    Shi et al.
    Cell Stem Cell, 2008;3:568
  4. Small-molecule histone methyltransferase inhibitors display rapid antimalarial activity against all blood stage forms in Plasmodium falciparum.
    Malmquist et al.
    Proc.Natl.Acad.Sci.U S A, 2012;109:16708

The citations listed below are publications that use Tocris products. Selected citations for BIX 01294 include:

Showing Results 1 - 1 of 1

  1. Activation of pluripotency genes in human fibroblast cells by a novel mRNA based approach.
    Authors: Plews Et al.
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