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TP-064

Chemical Structure : TP-064

CAS No.: 2080306-20-1

TP-064 (TP064)

Catalog No.: PC-63546Not For Human Use, Lab Use Only.

TP-064 is a potent, selective, and cell-active inhibitor of PRMT4 with IC50 of <10 nM and Kd of 7.1 nM, shows high selectivity (>100-fold) for PRMT4 over other PRMTs.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

TP-064 is a potent, selective, and cell-active inhibitor of PRMT4 with IC50 of <10 nM and Kd of 7.1 nM.
TP-064  shows high selectivity (>100-fold) for PRMT4 over other PRMTs.
TP-064  reduces dimethylation of BAF155 (IC50=340±30 nM) and MED12 (IC50=43±10 nM) in a dose-dependent manner in cell-baed assays.
TP-064  inhibits the proliferation of a subset of multiple myeloma cell lines (NCI-H929, RPMI8226, Cell IC50 of 379 and 886 nM, respectively) with affected cells arrested in G1 phase of the cell cycle, but has no effect on acute myeloid leukemia, colon cancer, or lung cancer cell lines.

Physicochemical Properties

M.Wt 458.606
Formula C28H34N4O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

250 mM in DMSO (114.65 mg/mL)

Chemical Name/SMILES

N-methyl-N-((2-(1-(2-(methylamino)ethyl)piperidin-4-yl)pyridin-4-yl)methyl)-3-phenoxybenzamide

References

1. Nakayama K, et al. Oncotarget. 2018 Apr 6;9(26):18480-18493.

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