TP-064

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

TP-064 是一种有效的、选择性的、具有细胞活性的 PRMT4 抑制剂，IC50 为 <10 nM，Kd 为 7.1 nM。

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.

TP-064 (1 μM; 72 hours) treatment reduces the proportion of NCI-H929 cells in S and G2/M phases while increasing the G1 phase fraction.TP-064 (0.03-3 μM; 72 hours) treatment reduces dimethyl-BAF155 level in a dose-dependent manner in both TP-064-sensitive and -insensitive cells.TP-064 (10 nM-10 μM; 6 days) treatment inhibits the growth of NCI-H929, RPMI8226, and MM.1R cells in a dose-dependent manner, but had no effect on acute myeloid leukemia, colon cancer, or lung cancer cell lines. Cell Cycle Analysis Cell Line:NCI-H929 cells Concentration:1 μM Incubation Time:72 hours Result:Induced G1 cell cycle arrest in NCI-H929 cells.Western Blot Analysis Cell Line:NCI-H929, KMS-27 and U266B1 cells.Concentration:0.03 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM Incubation Time:72 hours Result:Dimethyl-BAF155 level was reduced.

TP-064 (10 mg/kg; i.p.; 3 times in 5 days) induces peritonitis-associated neutrophilia in C57BL/6 mice.

TP064

Chromatin/Epigenetic

HMTase

HMTase

——

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2080306-20-1

458.606

C28H34N4O2

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (272.57 mM)

O=C(N(C)CC1=CC(C2CCN(CCNC)CC2)=NC=C1)C3=CC=CC(OC4=CC=CC=C4)=C3

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

(-20℃)

With Ice Pack

≥ 2 years