BIX 01294

Cat. No. 3364

BIX 01294 C28H38N6O2.3HCl [1392399-03-9]

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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.

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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Malmquist et al (2012) Small-molecule histone methyltransferase inhibitors display rapid antimalarial activity against all blood stage forms in Plasmodium falciparum. Proc.Natl.Acad.Sci.U S A 109 16708. PMID: 23011794.

Chang et al (2009) Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294. Nat.Struct.Mol.Biol. 16 312. PMID: 19219047.

Shi et al (2008) Induction of pluripotent stem cells from mouse embryonic fibroblasts by Oct4 and Klf4 with small-molecule compounds. Cell Stem Cell 3 568. PMID: 18983970.

Kubicek et al (2007) Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase. Mol.Cell 25 473. PMID: 17289593.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for BIX 01294 include:

Plews et al (2011) Activation of pluripotency genes in human fibroblast cells by a novel mRNA based approach. Diabetes 5 e14397. PMID: 21209933.

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Keywords: BIX 01294, supplier, G9a-like, protein, and, G9a, histone, lysine, methyltransferases, HMTases, inhibitors, inhibits, BIX01294, stem, cells, epigenetics, Tocris Bioscience, Lysine Methyltransferase Inhibitor products

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