2080306-20-1

2080306-20-1 structure

Name: TP 064
Chemical Name: N-Methyl-N-[(2-{1-[2-(methylamino)ethyl]-4-piperidinyl}-4-pyridinyl)methyl]-3-phenoxybenzamide
CAS Number: 2080306-20-1
Molecular Formula: C₂₈H₃₄N₄O₂
Molecular Weight: 458.595
Catalog: Signaling Pathways Epigenetics Histone Methyltransferase
Create Date: 2020-01-11 16:46:57
Modify Date: 2024-01-10 11:58:50
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; reduces dimethylation of BAF155 (IC50=340±30 nM) and MED12 (IC50=43±10 nM) in a dose-dependent manner in cell-baed assays; 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.

Name	N-Methyl-N-[(2-{1-[2-(methylamino)ethyl]-4-piperidinyl}-4-pyridinyl)methyl]-3-phenoxybenzamide
Synonyms	N-Methyl-N-[(2-{1-[2-(methylamino)ethyl]-4-piperidinyl}-4-pyridinyl)methyl]-3-phenoxybenzamide Benzamide, N-methyl-N-[[2-[1-[2-(methylamino)ethyl]-4-piperidinyl]-4-pyridinyl]methyl]-3-phenoxy-

Description	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; reduces dimethylation of BAF155 (IC50=340±30 nM) and MED12 (IC50=43±10 nM) in a dose-dependent manner in cell-baed assays; 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.
References	References 1. Nakayama K, et al. Oncotarget. 2018 Apr 6;9(26):18480-18493. View Related Products by Target Histone Methyltransferase (HMTase)