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

TP-064 

Cat. No.: HY-114965 Purity: 98.35%
COA 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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5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
50 mg USD 620 In-stock
Estimated Time of Arrival: December 31
100 mg USD 990 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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1 Publications Citing Use of MCE TP-064

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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.
SMILES

O=C(C1=CC=CC(OC2=CC=CC=C2)=C1)N(CC3=CC(C4CCN(CC4)CCNC)=NC=C3)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (272.57 mM; ultrasonic and warming and heat to 60°C)

H2O : ≥ 50 mg/mL (109.03 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1805 mL 10.9027 mL 21.8055 mL
5 mM 0.4361 mL 2.1805 mL 4.3611 mL
10 mM 0.2181 mL 1.0903 mL 2.1805 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.54 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.54 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.54 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 98.35%

References
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Product Name:
TP-064
Cat. No.:
HY-114965
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