BIX 01294

Pricing Availability Delivery Time Qty
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 (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.

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 60 100
water 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 solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

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

Safety Datasheet

References

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


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View Related Products by Product Action

View all Lysine Methyltransferase Inhibitors

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.

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Literature in this Area

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.

Pathways for BIX 01294

Protocols

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