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Submit ReviewBIX 01294
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)
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)
External Portal Information for BIX 01294
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 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.
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 Data 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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Product Datasheets for BIX 01294
References for BIX 01294
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
Barili et al (2020) Targeting p53 and histone methyltransferases restores exhausted CD8+ T cells in HCV infection. Nat.Commun. 11 604 PMID: 32001678
If you know of a relevant reference for BIX 01294, please let us know.
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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, CD8+, T, exhaustion, exhausted, viral, infections, Stem, Cell, Reprogramming, Lysine, Methyltransferases, G9a/GLP, 3364, Tocris Bioscience
4 Citations for BIX 01294
Citations are publications that use Tocris products. Selected citations for BIX 01294 include:
Li et al (2018) Epigenetic control of IL-23 expression in keratinocytes is important for chronic skin inflammation. Nat Commun 9 1420 PMID: 29650963
Plews et al (2011) Activation of pluripotency genes in human fibroblast cells by a novel mRNA based approach. Diabetes 5 e14397 PMID: 21209933
Bellamy et al (2020) Increased Efficacy of Histone Methyltransferase G9a Inhibitors Against MYCN-Amplified Neuroblastoma. Front Oncol 10 PMID: 32537432
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
Do you know of a great paper that uses BIX 01294 from Tocris? Please let us know.
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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* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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 in Cancer Poster
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.