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Submit ReviewA 366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor (IC50 = 3.3 nM). Exhibits >1000-fold selectivity for G9a/GLP over 21 other methyltransferases. Decreases levels of lysine 9 dimethylation on histone H3 (H3K9Me2) in PC3 cells.
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the A 366 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 A 366 is reviewed on the chemical probes website.
A 366 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。
分子量 | 329.44 |
公式 | C19H27N3O2 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1527503-11-2 |
PubChem ID | 76285486 |
InChI Key | BKCDJTRMYWSXMC-UHFFFAOYSA-N |
Smiles | COC1=C(OCCCN4CCCC4)C=C(N=C(N)C32CCC3)C2=C1 |
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 | |||
1eq. HCl | 32.94 | 100 | |
DMSO | 32.94 | 100 |
以下数据基于产品分子量 329.44。 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 | 3.04 mL | 15.18 mL | 30.35 mL |
5 mM | 0.61 mL | 3.04 mL | 6.07 mL |
10 mM | 0.3 mL | 1.52 mL | 3.04 mL |
50 mM | 0.06 mL | 0.3 mL | 0.61 mL |
参考文献是支持产品生物活性的出版物。
Sweis et al (2014) Discovery and development of potent and selective inhibitors of histone methyltransferase G9a. ACS Med.Chem.Lett. 5 205 PMID: 24900801
Scheer et al (2019) A chemical biology toolbox to study protein methyltransferases and epigenetic signaling. Nat.Commun. 10 19 PMID: 30604761
If you know of a relevant reference for A 366, please let us know.
关键词: A 366, A 366 supplier, A366, G9a, histone, methyltransferases, potent, selective, lysine, GLP, sgc, Lysine, Methyltransferases, G9a/GLP, 5163, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 A 366 的部分引用包括:
Xin et al (2019) Pharmacological Targeting of STK19 Inhibits Oncogenic NRAS-Driven Melanomagenesis. Cell 176 1113-1127.e16 PMID: 30712867
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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.
This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.