BIX 01294

Catalog # Availability Size / Price Qty
3364/10
3364/50
BIX 01294 | CAS No. 1392399-03-9 | Lysine Methyltransferase Inhibitors
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Description: GLP and G9a inhibitor

Chemical Name: 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine trihydrochloride

Purity: ≥98%

Product Details
Citations (3)
Reviews

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. 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
  2. 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
  3. BIX-01294 inhibits oncoproteins NSD1, NSD2, and NSD3.
    Morishita et al.
    Med.Chem.Res., 2017;26:2038
  4. Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase.
    Kubicek et al.
    Mol.Cell, 2007;25:473
  5. Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294.
    Chang et al.
    Nat.Struct.Mol.Biol., 2009;16:312

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Citations for BIX 01294

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

3 Citations: Showing 1 - 3

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