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说明： Potent and selective G9a and GLP inhibitor
化学名： 2-(4,4-Difluoro-1-piperidinyl)-6-methoxy-N-[1-(1-methylethyl)-4-piperidinyl]-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine
纯度： ≥99% (HPLC)
生物活性 for UNC 0642
UNC 0642 is a potent and selective G9a and GLP histone lysine methyltransferase inhibitor (IC50 < 2.5 nM) that exhibits >2,000-fold selectivity for G9a and GLP over PRC2-EZH2 and >20,000-fold selectivity over other methyltransferases. UNC 0642 reduces H3K9 dimethylation levels in MDA-MB-231 cells (IC50 = 110 nM), and displays modest brain penetration in vivo.
许可信息
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the UNC 0642 probe summary on the SGC website.
External Portal Information for UNC 0642
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of UNC0642 is reviewed on the chemical probes website.
化合物库 for UNC 0642
UNC 0642 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 UNC 0642
| 分子量 | 546.7 |
| 公式 | C29H44F2N6O2 |
| 储存 | Store at -20°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 1481677-78-4 |
| PubChem ID | 53315878 |
| InChI Key | RNAMYOYQYRYFQY-UHFFFAOYSA-N |
| Smiles | CC(C)N(CC4)CCC4NC1=C2C(C=C(OCCCN3CCCC3)C(OC)=C2)=NC(N5CCC(F)(F)CC5)=N1 |
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 UNC 0642
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 54.67 | 100 | |
| 1eq. HCl | 27.34 | 50 |
制备储备液 for UNC 0642
以下数据基于产品分子量 546.7。 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 | 1.83 mL | 9.15 mL | 18.29 mL |
| 5 mM | 0.37 mL | 1.83 mL | 3.66 mL |
| 10 mM | 0.18 mL | 0.91 mL | 1.83 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.37 mL |
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产品说明书 for UNC 0642
参考文献 for UNC 0642
参考文献是支持产品生物活性的出版物。
Liu et al (2013) Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP. J.Med.Chem. 56 8931 PMID: 24102134
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 UNC 0642, please let us know.
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关键词: UNC 0642, UNC 0642 supplier, UNC0642, potent, selective, G9a, GLP, histone, lysine, methyltransferase, inhibits, inhibitors, HMTs, HMTases, epigenetics, modifications, H3K9, H3K9me2, sgc, Lysine, Methyltransferases, G9a/GLP, 5132, Tocris Bioscience
3 篇 UNC 0642 的引用文献
引用文献是使用了 Tocris 产品的出版物。 UNC 0642 的部分引用包括：
Bellamy et al (2020) Increased Efficacy of Histone Methyltransferase G9a Inhibitors Against MYCN-Amplified Neuroblastoma Front Oncol 10 PMID: 32537432
Xi et al (2022) EHMT2 methyltransferase governs cell identity in the lung and is required for KRAS G12D tumor development and propagation. Elife 11 PMID: 35983994
Xin et al (2019) Pharmacological Targeting of STK19 Inhibits Oncogenic NRAS-Driven Melanomagenesis. Cell 176 1113-1127.e16 PMID: 30712867
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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
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.
Epigenetics in Cancer Poster
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.