BIX 01294

Name: BIX 01294
Brand: Tocris Bioscience
SKU: 3364

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

Citations (14)

COA / SDS

GLP and G9a inhibitor

Key Product Details

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%

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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.

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

Technical Data for BIX 01294

Formula	C₂₈H₃₈N₆O₂.3HCl
Storage	Desiccate at RT
Purity	≥98%
CAS Number	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.

Solubility for BIX 01294

Solubility

Soluble Soluble to 100 mM in water and to 100 mM in DMSO

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References for BIX 01294

References are publications that support the biological activity of the product.

Matthew N Svalina IGF1R as a Key Target in High Risk, Metastatic Medulloblastoma Sci Rep, 2016;6(0):27012. 2016 PMID: 27255663
Shi et al. Induction of pluripotent stem cells from mouse embryonic fibroblasts by Oct4 and Klf4 with small-molecule compounds. Cell Stem Cell., 2008;3:568 PMID: 18983970
Malmquist et al. 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;109:16708 PMID: 23011794
Morishita et al. BIX-01294 inhibits oncoproteins NSD1, NSD2, and NSD3. Med.Chem.Res., 2017;26:2038
Kubicek et al. Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase. Mol.Cell, 2007;25:473 PMID: 17289593
Chang et al. Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294. Nat.Struct.Mol.Biol., 2009;16:312 PMID: 19219047
Barili et al. Targeting p53 and histone methyltransferases restores exhausted CD8+ T cells in HCV infection. Nat.Commun., 2020;11:604 PMID: 32001678

BIX 01294

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

Key Product Details

Biological Activity for BIX 01294

Technical Data for BIX 01294

Solubility for BIX 01294

Dilution Calculator

Reconstitution Calculator

References for BIX 01294

Product Documents for BIX 01294

COA

Certificate of Analysis

SDS

CONTACT INFORMATION

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