1. Epigenetics
  2. Histone Methyltransferase
  3. TP-064

TP-064 

Cat. No.: HY-114965
Handling Instructions

TP-064 is a potent and selective proteinarginine methyltransferase 4 (PRMT4; CARM1) inhibitor (IC50 <10 nM). TP-064 inhibits dimethylation of BAF155 (IC50 of 340 nM) and MED12 (IC50 of 43 nM). TP-064 is inactive against the other family members except for PRMT6 (IC50 of 1.3 μM). TP-064 has anticancer activities.

For research use only. We do not sell to patients.

TP-064 Chemical Structure

TP-064 Chemical Structure

CAS No. : 2080306-20-1

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Description

TP-064 is a potent and selective proteinarginine methyltransferase 4 (PRMT4; CARM1) inhibitor (IC50 <10 nM). TP-064 inhibits dimethylation of BAF155 (IC50 of 340 nM) and MED12 (IC50 of 43 nM). TP-064 is inactive against the other family members except for PRMT6 (IC50 of 1.3 μM). TP-064 has anticancer activities[1].

IC50 & Target[1]

PRMT4

<10 nM (IC50)

PRMT6

1300 μM (IC50)

In Vitro

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[1].
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[1].
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

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[1]

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.
In Vivo

TP-064 (10 mg/kg; i.p.; 3 times in 5 days) induces peritonitis-associated neutrophilia in C57BL/6 mice[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

458.60

Formula

C₂₈H₃₄N₄O₂

CAS No.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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TP-064
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HY-114965
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