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Submit ReviewTP 064
Description: Potent and selective PRMT 4 inhibitor
Chemical Name: N-Methyl-N-((2-(1-(2-(methylamino)ethyl)piperidin-4-yl)pyridin-4-yl)methyl)-3-phenoxybenzamide
Purity: ≥98% (HPLC)
Biological Activity for TP 064
TP 064 is a 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. TP 064 can be used in vivo. TP 064 inhibits the monocyte/macrophage-driven inflammation in ex vivo.
To request the negative control for TP 064, please fill out the TP 064N request form on the SGC website..
Licensing Information
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.
Compound Libraries for TP 064
TP 064 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
Technical Data for TP 064
| M. Wt | 458.6 |
| Formula | C28H34N4O2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2080306-20-1 |
| PubChem ID | 122707126 |
| InChI Key | VUIITYLFSAXKIQ-UHFFFAOYSA-N |
| Smiles | O=C(N(C)CC1=CC(C2CCN(CCNC)CC2)=NC=C1)C3=CC=CC(OC4=CC=CC=C4)=C3 |
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 TP 064
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1eq. HCl | 45.86 | 100 | |
| DMSO | 45.86 | 100 |
Preparing Stock Solutions for TP 064
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 |
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Product Datasheets for TP 064
References for TP 064
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
Zhang et al (2021) PRMT4 inhibitor TP-064 inhibits the pro-inflammatory macrophage lipopolysaccharide response in vitro and ex vivo and induces peritonitis-associated neutrophilia in vivo. Biochim.Biophys.Acta Mol.Basis Dis. 1867 166212 PMID: 34311083
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
9 Citations for TP 064
Citations are publications that use Tocris products. Selected citations for TP 064 include:
Zhang et al (2021) PRMT4 inhibitor TP-064 inhibits the pro-inflammatory macrophage lipopolysaccharide response in vitro and ex vivo and induces peritonitis-associated neutrophilia in vivo. Biochim.Biophys.Acta Mol.Basis Dis. 1867 166212 PMID: 34311083
Yingze et al (2021) Endotoxin stabilizes protein arginine methyltransferase 4 (PRMT4) protein triggering death of lung epithelia. Cell Death Dis 12 828 PMID: 34480022
Mark T et al (2021) CARM1 regulates replication fork speed and stress response by stimulating PARP1. Mol Cell 81 784-800.e8 PMID: 33412112
Clemons et al (2022) Protein arginine methyltransferase 4 modulates nitric oxide synthase uncoupling and cerebral blood flow in Alzheimer's disease. J Cell Physiol 10 jcp.30858 PMID: 36036549
Yingze et al (2023) Protein arginine N-methyltransferase 4 (PRMT4) contributes to lymphopenia in experimental sepsis. Thorax 78 383-393 PMID: 35354645
Lauren E et al (2022) Arginine methylation of BRD4 by PRMT2/4 governs transcription and DNA repair. Sci Adv 8 eadd8928 PMID: 36475791
Mark T et al (2022) Pan-methylarginine antibody generation using PEG linked GAR motifs as antigens. Methods 200 80-86 PMID: 34107353
Clemons et al (2022) Protein arginine methyltransferase 4 modulates nitric oxide synthase uncoupling and cerebral blood flow in Alzheimer's disease J Cell Physiol PMID: 36036549
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* your copy today!
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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.