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Potent and selective PRMT4 inhibitor; inhibits methylation of H3 (1-25) and MED12 (IC50 values are <10 and 43 nM, respectively). Exhibits >100-fold selectivity over other histone methyltransferases and non-epigenetic targets. Inhibits proliferation of certain multiple myeloma cell lines, arresting cells in G1 phase.
To request the negative control for TP 064, please fill out the TP 064N request form on the SGC website.
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the TP 064 probe summary on the SGC website.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 458.6. 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||2.18 mL||10.9 mL||21.81 mL|
|5 mM||0.44 mL||2.18 mL||4.36 mL|
|10 mM||0.22 mL||1.09 mL||2.18 mL|
|50 mM||0.04 mL||0.22 mL||0.44 mL|
References are publications that support the biological activity of the product.
Nakayama et al (2018) TP-064, a potent and selective small molecule inhibitor of PRMT4 for multiple myeloma. Oncotarget 9 18480 PMID: 29719619
Scheer et al (2019) A chemical biology toolbox to study protein methyltransferases and epigenetic signaling. Nat.Commun. 10 19 PMID: 30604761
If you know of a relevant reference for TP 064, please let us know.
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Keywords: TP 064, TP 064 supplier, TP064, Potent, allosteric, inhibitors, inhibits, of, protein, arginine, methyltransferase, 4, PRMT4, methylation, Protein, Arginine, Methyltransferases, 6008, Tocris Bioscience
1 Citation for TP 064
Citations are publications that use Tocris products. Selected citations for TP 064 include:
Zhong et al (2018) CARM1 Methylates GAPDH to Regulate Glucose Metabolism and Is Suppressed in Liver Cancer. Cell Rep 24 3207 PMID: 30232003
Do you know of a great paper that uses TP 064 from Tocris? Please let us know.
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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.
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 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:
- DNA Methyltransferases
- Histone Deacetylases
- Histone Demethylases
- Histone Methyltransferases