BIX 01294

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Cat.No. 3364 - BIX 01294 | C28H38N6O2.3HCl | CAS No. 1392399-03-9
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)
Datasheet
Citations (3)
Reviews
Protocols (1)
Literature

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. Also inhibits H3K36 methylation by oncoproteins NSD1, NSD2 and NSD3 (IC50 values are 40 - 112 μM).

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.

Compound Libraries

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

Technical Data

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 Data

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

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 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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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

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

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

Morishita et al (2017) BIX-01294 inhibits oncoproteins NSD1, NSD2, and NSD3. Med.Chem.Res. 26 2038


If you know of a relevant reference for BIX 01294, please let us know.

View Related Products by Product Action

View all G9a/GLP Inhibitors

Keywords: BIX 01294, BIX 01294 supplier, G9a-like, protein, and, G9a, histone, lysine, methyltransferases, HMTases, inhibitors, inhibits, BIX01294, stem, cells, epigenetics, oncoproteins, NSD1, NSD2, NSD3, Reprogramming, Lysine, Methyltransferases, G9a/GLP, 3364, Tocris Bioscience

3 Citations for BIX 01294

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

Li et al (2019) Negative regulation of p53-induced senescence by N-WASP is crucial for DMBA/TPA-induced skin tumor formation. Cancer Res PMID: 30894371

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

Li et al (2018) Epigenetic control of IL-23 expression in keratinocytes is important for chronic skin inflammation. Nat Commun 9 1420 PMID: 29650963


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Protocols for BIX 01294

The following protocol features additional information for the use of BIX 01294 (Cat. No. 3364).

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Epigenetics

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.

Epigenetics

Epigenetics Research Bulletin

Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:

  • Bromodomains
  • DNA Methyltransferases
  • Histone Deacetylases
  • Histone Demethylases
  • Histone Methyltransferases
Epigenetics in Cancer

Epigenetics in Cancer Poster

Adapted from the 2015 Cancer Product Guide Edition 3, this poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.