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TP 064

Catalog #: 6008
9 Citations Datasheet
Catalog # Availability Size / Price Qty
6008/10
6008/50
TP 064 | CAS No. 2080306-20-1 | Protein Arginine Methyltransferase Inhibitors
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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%

Product Details
Citations (9)
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

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..

Technical Data

M.Wt:
458.6
Formula:
C28H34N4O2
Solubility:
Soluble to 100 mM in 1eq. HCl and to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
2080306-20-1

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.

Additional Information

Licensing Caveats:
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.

Product Datasheets

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Citations for TP 064

The citations listed below are publications that use Tocris products. Selected citations for TP 064 include:

9 Citations: Showing 1 - 9

  1. Protein arginine N-methyltransferase 4 (PRMT4) contributes to lymphopenia in experimental sepsis.
    Authors: Yingze Et al.
    Thorax  2023;78:383-393
  2. Arginine methylation of BRD4 by PRMT2/4 governs transcription and DNA repair.
    Authors: Lauren E Et al.
    Sci Adv  2022;8:eadd8928
  3. Pan-methylarginine antibody generation using PEG linked GAR motifs as antigens.
    Authors: Mark T Et al.
    Methods  2022;200:80-86
  4. Protein arginine methyltransferase 4 modulates nitric oxide synthase uncoupling and cerebral blood flow in Alzheimer's disease.
    Authors: Clemons Et al.
    J Cell Physiol  2022;10:jcp.30858
  5. Protein arginine methyltransferase 4 modulates nitric oxide synthase uncoupling and cerebral blood flow in Alzheimer's disease
    Authors: Clemons Et al.
    J Cell Physiol  2022;
  6. CARM1 regulates replication fork speed and stress response by stimulating PARP1.
    Authors: Mark T Et al.
    Mol Cell  2021;81:784-800.e8
  7. PRMT4 inhibitor TP-064 inhibits the pro-inflammatory macrophage lipopolysaccharide response in vitro and ex vivo and induces peritonitis-associated neutrophilia in vivo.
    Authors: Zhang Et al.
    Biochim.Biophys.Acta Mol.Basis Dis.  2021;1867:166212
  8. Endotoxin stabilizes protein arginine methyltransferase 4 (PRMT4) protein triggering death of lung epithelia.
    Authors: Yingze Et al.
    Cell Death Dis  2021;12:828
  9. CARM1 Methylates GAPDH to Regulate Glucose Metabolism and Is Suppressed in Liver Cancer.
    Authors: Zhong Et al.
    Cell Rep  2018;24:3207

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