BIX 01294

Key Product Details

Product Description

BIX 01294 is a 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). Restores metabolic and antiviral function in exhausted CD8⁺ T cells from patients with chronic HCV infection. Promotes conversion of fibroblasts to cardiomyocytes as part of 9C cocktail (see our protocol below).

For more information about how BIX 01294 trihydrochloride may be used, see our protocol: Converting Fibroblasts into Cardiomyocytes (9C Cocktail)

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.

Product Specifications for BIX 01294

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for BIX 01294

The following data is based on the product molecular weight 600.02.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

3 2 1 Recalculate

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

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 16 publications citing the usage of this product.

• Barili Targeting p53 and histone methyltransferases restores exhausted CD8+ T cells in HCV infection. Nat.Commun. 2020 PMID: 32001678
• Morishita BIX-01294 inhibits oncoproteins NSD1, NSD2, and NSD3. Med.Chem.Res.
• Malmquist Small-molecule histone methyltransferase inhibitors display rapid antimalarial activity against all blood stage forms in Plasmodium falciparum. Proc.Natl.Acad.Sci.U.S.A. 2012 PMID: 23011794
• Shi Induction of pluripotent stem cells from mouse embryonic fibroblasts by Oct4 and Klf4 with small-molecule compounds. Cell Stem Cell 2008 PMID: 18983970
• Chang Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294. Nat.Struct.Mol.Biol. 2009 PMID: 19219047
• Kubicek Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase. Mol.Cell 2007 PMID: 17289593

Product Documents for BIX 01294