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Submit ReviewGSK 343
说明： Potent and selective SAM-competitive EZH2 inhibitor
化学名： N-[(1,2-Dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[2-(4-methyl-1-piperazinyl)-4-pyridinyl]-1H-indazole-4-carboxamide
纯度： ≥98% (HPLC)
生物活性 for GSK 343
GSK 343 is a potent and selective SAM-competitive EZH2 inhibitor (IC50 = 4 nM), that exhibits >60 fold selectivity for EZH2 over EZH1 and a range of other methyltransferases. GSK 343 decreases H3K27me3 levels in breast cancer cells and inhibits proliferation of prostate cancer cell lines in vitro.
许可信息
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the GSK343 probe summary on the SGC website.
External Portal Information for GSK 343
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of GSK 343 is reviewed on the chemical probes website.
技术数据 for GSK 343
| 分子量 | 541.69 |
| 公式 | C31H39N7O2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1346704-33-3 |
| PubChem ID | 71268957 |
| InChI Key | ULNXAWLQFZMIHX-UHFFFAOYSA-N |
| Smiles | CCCC1=C(C(NC(C)=C1)=O)CNC(C2=C3C=NN(C3=CC(C4=CC=NC(N5CCN(CC5)C)=C4)=C2)C(C)C)=O |
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 GSK 343
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 10.83 | 20 温和加热 |
制备储备液 for GSK 343
以下数据基于产品分子量 541.69。 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 |
|---|---|---|---|
| 0.2 mM | 9.23 mL | 46.15 mL | 92.3 mL |
| 1 mM | 1.85 mL | 9.23 mL | 18.46 mL |
| 2 mM | 0.92 mL | 4.62 mL | 9.23 mL |
| 10 mM | 0.18 mL | 0.92 mL | 1.85 mL |
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产品说明书 for GSK 343
参考文献 for GSK 343
参考文献是支持产品生物活性的出版物。
Verma et al (2012) Identification of potent, selective, cell-active inhibitors of the histone lysine methyltransferase EZH2. ACS Med.Chem.Lett. 3 1091 PMID: 24900432
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 GSK 343, please let us know.
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关键词: GSK 343, GSK 343 supplier, GSK343, potent, and, selective, EZH2, inhibitors, inhibits, lysine, methyltransferase, PRC2, polycomb, repressive, complex, 2, Lysine, Methyltransferases, 6128, Tocris Bioscience
1 篇 GSK 343 的引用文献
引用文献是使用了 Tocris 产品的出版物。 GSK 343 的部分引用包括：
Karin et al (2021) A distinct metabolic response characterizes sensitivity to EZH2 inhibition in multiple myeloma. Cell Death Dis 12 167 PMID: 33579905
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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.
Stem Cells Scientific Review
Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.
Cancer Metabolism Poster
This poster summarizes the main metabolic pathways in cancer cells and highlights potential targets for cancer therapeutics. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways providing potential cancer therapeutic targets.
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.
Stem Cells Poster
Written by Rebecca Quelch and Stefan Przyborski from Durham University (UK), this poster describes the isolation of pluripotent stem cells, their maintenance in culture, differentiation, and the generation and potential uses of organoids.