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. Also inhibits H3K36 methylation by oncoproteins NSD1, NSD2 and NSD3 (IC50 values are 40 - 112 μM).
External Portal Information
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of BIX-01294 is reviewed on the chemical probes website.
Technical Data
  • M.Wt:
    600.02
  • Formula:
    C28H38N6O2.3HCl
  • Solubility:
    Soluble to 100 mM in water and to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Desiccate at RT
  • CAS No:
    1392399-03-9
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
  5. BIX-01294 inhibits oncoproteins NSD1, NSD2, and NSD3.
    Morishita et al.
    Med.Chem.Res., 2017;26:2038
Citations:

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

1 Citations: Showing 1 - 1

  1. Activation of pluripotency genes in human fibroblast cells by a novel mRNA based approach.
    Authors: Plews Et al.
    Diabetes 2011;5:e14397

Have you used BIX 01294?

Submit a review and receive a $25US/€18/£15/$25CAN amazon gift card if you include an image - $10US/€7/£6/$10CAN Amazon card for reviews without an image. Limited to verified customers in USA, Canada and Europe.

Tocris Bioscience is the leading supplier of novel and exclusive tools for life science research with over 30 years' experience in the industry. Tocris is a Bio-Techne brand.

Order Details

Note:

Contact Information

Calculators

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

R&D Systems Guarantee

Feedback

Customer Information