BIX 01294

Name: BIX 01294
Brand: Tocris Bioscience
SKU: 3364

Tocris Bioscience, part of Bio-Techne | Catalog # 3364

Citations (21)

COA / SDS

GLP and G9a inhibitor

Key Product Details

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% (HPLC)
Molecular Weight:	600.02

View Full Technical Details for BIX 01294

Technical Data
Citations

Biological Activity for BIX 01294

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)

Compound Libraries for BIX 01294

BIX 01294 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Epigenetics Library and Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.

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 for BIX 01294

M. Wt	600.02
Formula	C₂₈H₃₈N₆O₂.3HCl
Storage	Desiccate at RT
Purity	≥98% (HPLC)
CAS Number	1392399-03-9
PubChem ID	46945860
InChi Key	FMURUEPQXKJIPS-UHFFFAOYSA-N
Smiles	CN(CCC3)CCN3C2=NC1=CC(OC)=C(OC)C=C1C(NC4CCN(CC5=CC=CC=C5)CC4)=N2.Cl.Cl.Cl

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.

Solubility for BIX 01294

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	water	60	100
	DMSO	60	100

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 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

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References for BIX 01294

References are publications that support the biological activity of the 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