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说明： Potent WDR5/MLL interaction inhibitor
化学名： 1-[[(2S)-5-[(Aminoiminomethyl)amino]-2-[[2-ethyl-2-[(2-methyl-1-oxopropyl)amino]-1-oxobutyl]amino]-1-oxopentyl]amino]-N-[bis(4-fluorophenyl)methyl]-cyclopentanecarboxamide trifluoroacetate
纯度： ≥95% (HPLC)
生物活性 for MM 102
MM 102 is a potent WDR5/MLL interaction inhibitor (IC50 = 2.4 nM). Inhibits MLL1 methyltransferase activity and MLL-1-induced HoxA9 and Meis-1 gene expression in leukemia cells expressing the MLL1-AF9 fusion gene. Also inhibits cell growth and induces apoptosis in leukemia cells harbouring MLL1 fusion proteins.
化合物库 for MM 102
MM 102 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 MM 102
| 分子量 | 783.83 |
| 公式 | C35H49F2N7O4.CF3CO2H |
| 储存 | Store at -20°C |
| 纯度 | ≥95% (HPLC) |
| CAS Number | 1883545-52-5 |
| PubChem ID | 71520620 |
| InChI Key | ZRKTWBXVGMHWHM-YCBFMBTMSA-N |
| Smiles | O=C(NC(C2=CC=C(F)C=C2)C1=CC=C(F)C=C1)C3(CCCC3)NC([C@@H](NC(C(CC)(CC)NC(C(C)C)=O)=O)CCCNC(N)=N)=O.OC(C(F)(F)F)=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 MM 102
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 66.98 | 100 |
制备储备液 for MM 102
以下数据基于产品分子量 783.83。 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 | 1.28 mL | 6.38 mL | 12.76 mL |
| 5 mM | 0.26 mL | 1.28 mL | 2.55 mL |
| 10 mM | 0.13 mL | 0.64 mL | 1.28 mL |
| 50 mM | 0.03 mL | 0.13 mL | 0.26 mL |
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产品说明书 for MM 102
参考文献 for MM 102
参考文献是支持产品生物活性的出版物。
Karatas et al (2013) High-affinity, small-molecule peptidomimetic inhibitors of MLL1/WDR5 protein-protein interaction. J.Am.Chem.Soc. 135 669 PMID: 23210835
If you know of a relevant reference for MM 102, please let us know.
关键词: MM 102, MM 102 supplier, MM102, Mixed, lineage, leukemia, 1, MLL1, WD, repeat-containing, protein, 5, WDR5, interaction, inhibitors, inhibits, leukaemia, WD40, 14173292483, 1417329_24_83, Lysine, Methyltransferases, 5307, Tocris Bioscience
2 篇 MM 102 的引用文献
引用文献是使用了 Tocris 产品的出版物。 MM 102 的部分引用包括：
Ilona et al (2019) Epigenetic stabilization of DC and DC precursor classical activation by TNFα contributes to protective T cell polarization. Sci Adv 5 eaaw9051 PMID: 31840058
Ayumu et al (2019) Inhibition of the H3K4 methyltransferase MLL1/WDR5 complex attenuates renal senescence in ischemia reperfusion mice by reduction of p16INK4a. Kidney Int 96 1162-1175 PMID: 31570196
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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.