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Submit ReviewGSK 126
说明： Very high affinity and selective EZH2 inhibitor
化学名： N-[(1,2-Dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-3-methyl-1-[(1S)-1-methylpropyl]-6-[6-(1-piperazinyl)-3-pyridinyl]-1H-indole-4-carboxamide
纯度： ≥98% (HPLC)
生物活性 for GSK 126
GSK 126 is a very high affinity and selective EZH2 inhibitor (Ki = 0.5 - 3 nM). Exhibits >150-fold selectivity for EZH2 over EZH1 and >1000-fold selectivity over 20 other human methyltransferases. Inhibits proliferation of B-cell lymphoma cell lines in vitro. Also inhibits H3K27Me3 and tumor growth in mice bearing BCL xenografts. Targeting p53 and histone methyltransferases restores exhausted CD8+ T cells in HCV infection. Promotes the transition of ESCs to feeder-free extended pluripotent stem (EPS) cells in combination with LCDM cocktail.
技术数据 for GSK 126
| 分子量 | 526.67 |
| 公式 | C31H38N6O2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1346574-57-9 |
| PubChem ID | 68210102 |
| InChI Key | FKSFKBQGSFSOSM-QFIPXVFZSA-N |
| Smiles | CC[C@@H](N1C=C(C2=C(C(NCC3=C(C=C(NC3=O)C)C)=O)C=C(C4=CN=C(N5CCNCC5)C=C4)C=C12)C)C |
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 126
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 2.63 | 5 温和加热 |
制备储备液 for GSK 126
以下数据基于产品分子量 526.67。 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 |
|---|---|---|---|
| 0.05 mM | 37.97 mL | 189.87 mL | 379.74 mL |
| 0.25 mM | 7.59 mL | 37.97 mL | 75.95 mL |
| 0.5 mM | 3.8 mL | 18.99 mL | 37.97 mL |
| 2.5 mM | 0.76 mL | 3.8 mL | 7.59 mL |
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产品说明书 for GSK 126
参考文献 for GSK 126
参考文献是支持产品生物活性的出版物。
McCabe et al (2012) EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations. Nature 492 108 PMID: 23051747
Barili et al (2020) Targeting p53 and histone methyltransferases restores exhausted CD8+ T cells in HCV infection. Nat.Commun. 11 604 PMID: 32001678
Zheng et al (2021) Derivation of feeder-free human extended pluripotent stem cells. Stem Cell Rep 16 1686 PMID: 34214484
If you know of a relevant reference for GSK 126, please let us know.
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关键词: GSK 126, GSK 126 supplier, GSK126, EZH2, inhibitors, inhibits, high, affinity, selective, enhancer, of, zeste, exhausted, T, cells, CD8+, exhaustion, chronic, infection, extended, pluripotent, stem, EPS, LCDM, ESCs, and, iPSC, 6790, Tocris Bioscience
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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.