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说明： Potent and selective EZH2/EZH1 inhibitor
化学名： N-[(1,2-Dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[6-[4-(1-methylethyl)-1-piperazinyl]-3-pyridinyl]-1H-indazole-4-carboxamide
纯度： ≥99% (HPLC)
生物活性 for UNC 1999
UNC 1999 is a potent and SAM-competitive EZH2/EZH1 lysine methyltransferase inhibitor (IC50 values are 10 and 45 nM, respectively). Selective for EZH2/EZH1 over a panel of other methyltransferases and non-epigenetic targets. Reduces H3K27me3 levels in vitro. Prolongs survival of MLL-AF9 bearing mice. Orally bioavailable.
Negative Control also available.
许可信息
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the UNC 1999 probe summary on the SGC website.
External Portal Information for UNC 1999
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of UNC 1999 is reviewed on the chemical probes website.
化合物库 for UNC 1999
UNC 1999 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 1999
| 分子量 | 569.74 |
| 公式 | C33H43N7O2 |
| 储存 | Store at +4°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 1431612-23-5 |
| PubChem ID | 72551585 |
| InChI Key | DPJNKUOXBZSZAI-UHFFFAOYSA-N |
| Smiles | CC(C)N1CCN(C2=NC=C(C3=CC(N(C(C)C)N=C4)=C4C(C(NCC5=C(CCC)C=C(C)NC5=O)=O)=C3)C=C2)CC1 |
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 1999
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| 1M HCl | 56.97 | 100 | |
| DMSO | 11.39 | 20 |
制备储备液 for UNC 1999
以下数据基于产品分子量 569.74。 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 | 1.76 mL | 8.78 mL | 17.55 mL |
| 5 mM | 0.35 mL | 1.76 mL | 3.51 mL |
| 10 mM | 0.18 mL | 0.88 mL | 1.76 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.35 mL |
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产品说明书 for UNC 1999
参考文献 for UNC 1999
参考文献是支持产品生物活性的出版物。
Konze et al (2013) An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem.Biol. 8 1324 PMID: 23614352
Xu et al (2015) Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia. Blood 125 346 PMID: 25395428
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 1999, please let us know.
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关键词: UNC 1999, UNC 1999 supplier, UNC1999, potent, selective, EZH2, EZH1, histone, methyltransferase, inhibitors, inhibits, UNC2400, sgc, PRC2, polycomb, repressive, complex, 2, Lysine, Methyltransferases, 4904, Tocris Bioscience
1 篇 UNC 1999 的引用文献
引用文献是使用了 Tocris 产品的出版物。 UNC 1999 的部分引用包括：
Chagraoui et al (2018) SCL/TAL1 cooperates with Polycomb RYBP-PRC1 to suppress alternative lineages in blood-fated cells. Nat Commun 9 5375 PMID: 30560907
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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.
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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.
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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.
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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.