TP-064
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MedKoo CAT#: 407418

CAS#: 2080306-20-1

Description: TP-064 is a potent and selective PRMT4 inhibitor. The in vitro activity of TP-064 includes inhibition of PRMT4 with IC50 < 10nM for methylation of H3 (1-25) and greater than 100-fold selectivity over other histone methyltransferases and non-epigenetic targets. In cellular assays, TP-064 inhibits the methylation of MED12 with IC50 = 43 nM.

Chemical Structure

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TP-064
CAS# 2080306-20-1
Instruction

Theoretical Analysis

MedKoo Cat#: 407418
Name: TP-064
CAS#: 2080306-20-1
Chemical Formula: C28H34N4O2
Exact Mass: 458.27
Molecular Weight: 458.606
Elemental Analysis: C, 73.33; H, 7.47; N, 12.22; O, 6.98

Price and Availability

Size Price Availability Quantity
5mg USD 255
10mg USD 395
25mg USD 695
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Synonym: TP-064; TP 064; TP064.

IUPAC/Chemical Name: N-Methyl-N-((2-(1-(2-(methylamino)ethyl)piperidin-4-yl)pyridin-4-yl)methyl)-3-phenoxybenzamide

InChi Key: VUIITYLFSAXKIQ-UHFFFAOYSA-N

InChi Code: InChI=1S/C28H34N4O2/c1-29-15-18-32-16-12-23(13-17-32)27-19-22(11-14-30-27)21-31(2)28(33)24-7-6-10-26(20-24)34-25-8-4-3-5-9-25/h3-11,14,19-20,23,29H,12-13,15-18,21H2,1-2H3

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

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 458.61 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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http://www.thesgc.org/chemical-probes/TP-064

A collaboration between Takeda and the SGC has resulted in the discovery of TP-064, the first potent, selective and cell active chemical probe for PRMT4. The in vitro activity of TP-064 includes inhibition of PRMT4 with IC50 < 10nM for methylation of H3 (1-25) and greater than 100-fold selectivity over other histone methyltransferases and non-epigenetic targets. In cellular assays, TP-064 inhibits the methylation of MED12 with IC50 = 43 nM.

A closely related compound, TP-064N, exhibits no activity in the biochemical and cellular assays, and is an ideal control compound for cellular studies.