TP 064

Pricing Availability   Qty
说明: Potent and selective PRMT 4 inhibitor
化学名: N-Methyl-N-((2-(1-(2-(methylamino)ethyl)piperidin-4-yl)pyridin-4-yl)methyl)-3-phenoxybenzamide
纯度: ≥98% (HPLC)
说明书
引用文献 (9)
评论
文献 (1)

生物活性 for TP 064

TP 064 is a potent and selective PRMT4 inhibitor; inhibits methylation of H3 (1-25) and MED12 (IC50 values are <10 and 43 nM, respectively). Exhibits >100-fold selectivity over other histone methyltransferases and non-epigenetic targets. Inhibits proliferation of certain multiple myeloma cell lines, arresting cells in G1 phase. TP 064 can be used in vivo. TP 064 inhibits the monocyte/macrophage-driven inflammation in ex vivo.

To request the negative control for TP 064, please fill out the TP 064N request form on the SGC website..

许可信息

This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the TP 064 probe summary on the SGC website.

化合物库 for TP 064

TP 064 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。

技术数据 for TP 064

分子量 458.6
公式 C28H34N4O2
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2080306-20-1
PubChem ID 122707126
InChI Key VUIITYLFSAXKIQ-UHFFFAOYSA-N
Smiles O=C(N(C)CC1=CC(C2CCN(CCNC)CC2)=NC=C1)C3=CC=CC(OC4=CC=CC=C4)=C3

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for TP 064

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
1eq. HCl 45.86 100
DMSO 45.86 100

制备储备液 for TP 064

以下数据基于产品分子量 458.6。 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.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 2.18 mL 10.9 mL 21.81 mL
5 mM 0.44 mL 2.18 mL 4.36 mL
10 mM 0.22 mL 1.09 mL 2.18 mL
50 mM 0.04 mL 0.22 mL 0.44 mL

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产品说明书 for TP 064

分析证书/产品说明书
选择另一批次:

参考文献 for TP 064

参考文献是支持产品生物活性的出版物。

Nakayama et al (2018) TP-064, a potent and selective small molecule inhibitor of PRMT4 for multiple myeloma. Oncotarget 9 18480 PMID: 29719619

Scheer et al (2019) A chemical biology toolbox to study protein methyltransferases and epigenetic signaling. Nat.Commun. 10 19 PMID: 30604761

Zhang et al (2021) PRMT4 inhibitor TP-064 inhibits the pro-inflammatory macrophage lipopolysaccharide response in vitro and ex vivo and induces peritonitis-associated neutrophilia in vivo. Biochim.Biophys.Acta Mol.Basis Dis. 1867 166212 PMID: 34311083


If you know of a relevant reference for TP 064, please let us know.

关键词: TP 064, TP 064 supplier, TP064, Potent, allosteric, inhibitors, inhibits, of, protein, arginine, methyltransferase, 4, PRMT4, methylation, Protein, Arginine, Methyltransferases, 6008, Tocris Bioscience

9 篇 TP 064 的引用文献

引用文献是使用了 Tocris 产品的出版物。 TP 064 的部分引用包括:

Zhang et al (2021) PRMT4 inhibitor TP-064 inhibits the pro-inflammatory macrophage lipopolysaccharide response in vitro and ex vivo and induces peritonitis-associated neutrophilia in vivo. Biochim.Biophys.Acta Mol.Basis Dis. 1867 166212 PMID: 34311083

Yingze et al (2021) Endotoxin stabilizes protein arginine methyltransferase 4 (PRMT4) protein triggering death of lung epithelia. Cell Death Dis 12 828 PMID: 34480022

Mark T et al (2021) CARM1 regulates replication fork speed and stress response by stimulating PARP1. Mol Cell 81 784-800.e8 PMID: 33412112

Clemons et al (2022) Protein arginine methyltransferase 4 modulates nitric oxide synthase uncoupling and cerebral blood flow in Alzheimer's disease. J Cell Physiol 10 jcp.30858 PMID: 36036549


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该领域的文献

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。


Epigenetics Scientific Review

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.