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.
|Storage||Desiccate at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 600.02. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.67 mL||8.33 mL||16.67 mL|
|5 mM||0.33 mL||1.67 mL||3.33 mL|
|10 mM||0.17 mL||0.83 mL||1.67 mL|
|50 mM||0.03 mL||0.17 mL||0.33 mL|
The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.
References are publications that support the products' biological activity.
Kubicek et al (2007) Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase. Mol.Cell 25 473 PMID: 17289593
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
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
If you know of a relevant reference for BIX 01294, please let us know.
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Keywords: G9a-like protein and G9a histone lysine methyltransferases HMTases inhibitors inhibits BIX01294 stem cells epigenetics Lysine Methyltransferases
1 Citation for BIX 01294
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
Do you know of a great paper that uses BIX 01294 from Tocris? If so please let us know.
Literature in this Area
Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.