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Submit ReviewMS 023 dihydrochloride is a potent and selective type I PRMT inhibitor (IC50 values are 8, 8, 30, 83 and 119 nM for PRMT6, PRMT8, PRMT1, PRMT4 and PRMT3, respectively). Exhibits no significant activity against type II and III PRMTs, PKMTs, DNMTs, KDMs and reader proteins. Reduces global arginine asymmetric dimethylation levels in vitro. Also inhibits and reduces TGF-β-activated kinase 1 expression and protein levels.
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the MS023 probe summary on the SGC website.
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of MS023 is reviewed on the chemical probes website.
分子量 | 360.32 |
公式 | C17H25N3O.2HCl |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1992047-64-9 |
PubChem ID | 121513886 |
InChI Key | HCNXCUFNZWGILO-UHFFFAOYSA-N |
Smiles | CC(C)OC1=CC=C(C2=CNC=C2CN(CCN)C)C=C1.Cl.Cl |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 36.03 | 100 | |
DMSO | 36.03 | 100 |
以下数据基于产品分子量 360.32。 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.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.78 mL | 13.88 mL | 27.75 mL |
5 mM | 0.56 mL | 2.78 mL | 5.55 mL |
10 mM | 0.28 mL | 1.39 mL | 2.78 mL |
50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
参考文献是支持产品生物活性的出版物。
Eram et al (2016) A potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases. ACS Chem.Biol. 11 772 PMID: 26598975
Scheer et al (2019) A chemical biology toolbox to study protein methyltransferases and epigenetic signaling. Nat.Commun. 11 19 PMID: 30604761
If you know of a relevant reference for MS 023 dihydrochloride, please let us know.
关键词: MS 023 dihydrochloride, MS 023 dihydrochloride supplier, MS023, dihydrochloride, potent, Type-1, selective, PRMT, inhibitors, inhibits, PRMT6, PRMT8, PRMT1, PRMT4, PRMT3, Protein, Arginine, Methyltransferases, 5713, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 MS 023 dihydrochloride 的部分引用包括:
Tang et al (2022) A genome-scale CRISPR screen reveals PRMT1 as a critical regulator of androgen receptor signaling in prostate cancer. Cell Rep. 38 110417 PMID: 35196489
Lu et al (2021) Pharmacologic modulation of RNA splicing enhances anti-tumor immunity. Cell PMID: 34171309
Choucair et al (2019) The arginine methyltransferase PRMT1 regulates IGF-1 signaling in breast cancer. Oncogene 38 4015 PMID: 30692633
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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。
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.