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SGC 0946

Cat. No. 4541 1 次引用 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Highly potent and selective DOT1L inhibitor; cell permeable
化学名： 1-[3-[[[(2R,3S,4R,5R)-5-(4-Amino-5-bromo-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxytetrahydrofuran-2-yl]methyl](isopropyl)amino]propyl]-3-[4-(2,2-dimethylethyl)phenyl]urea
纯度： ≥99% (HPLC)
说明书
引用文献 (1)
评论
实验方案 (1)
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for SGC 0946

SGC 0946 is a highly potent DOT1L methyltransferase inhibitor (Kd = 0.06 nM, IC50 = 0.3 nM in a radioactive assay); blocks H3K79 methylation in A431 cells and MCF10A cells. Inactive at 12 histone methyltransferases and DNMT1. Selectively kills cells transformed with the MLL-AF9 fusion oncogene in an in vitro model of leukemia; lowers levels of MLL target genes HOXA9 and Meis1.

To request the negative control for SGC0946, please fill out the SGC0649 request form on the SGC website.

For more information about how SGC 0946 may be used, see our protocol: Highly Efficient Generation of CiPSCs from MEFs

许可信息

This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the SGC 0946 probe summary on the SGC website.

External Portal Information for SGC 0946

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of SGC 0946 is reviewed on the chemical probes website.

化合物库 for SGC 0946

SGC 0946 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 SGC 0946

分子量 618.57
公式 C28H40BrN7O4
储存 Store at -20°C
纯度 ≥99% (HPLC)
CAS Number 1561178-17-3
PubChem ID 56962337
InChI Key IQCKJUKAQJINMK-HUBRGWSESA-N
Smiles O[C@H]([C@H](O)[C@@H](CN(C(C)C)CCCNC(NC4=CC=C(C(C)(C)C)C=C4)=O)O3)[C@@H]3N1C2=C(C(N)=NC=N2)C(Br)=C1

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 SGC 0946

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 61.86 100
ethanol 61.86 100

制备储备液 for SGC 0946

以下数据基于产品分子量 618.57。 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.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 1.62 mL 8.08 mL 16.17 mL
5 mM 0.32 mL 1.62 mL 3.23 mL
10 mM 0.16 mL 0.81 mL 1.62 mL
50 mM 0.03 mL 0.16 mL 0.32 mL

Molarity Calculator

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Reconstitution Calculator

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Dilution Calculator

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产品说明书 for SGC 0946

分析证书/产品说明书
选择另一批次：
化学品安全技术说明书

参考文献 for SGC 0946

参考文献是支持产品生物活性的出版物。

Yu et al (2012) Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat.Commun. 3 1288 PMID: 23250418

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 SGC 0946, please let us know.

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关键词: SGC 0946, SGC 0946 supplier, SGC0946, epigenetics, DOT1L, histone, protein, methyltransferase, PKMTs, H3K79me, potent, selective, inhibitors, inhibits, leukemia, MLL, target, genes, Lysine, Methyltransferases, Other, 4541, Tocris Bioscience

1 篇 SGC 0946 的引用文献

引用文献是使用了 Tocris 产品的出版物。 SGC 0946 的部分引用包括：

Christopher J et al (2022) Pharmacologic Targeting of TFIIH Suppresses KRAS-Mutant Pancreatic Ductal Adenocarcinoma and Synergizes with TRAIL. Cancer Res 82 3375-3393 PMID: 35819261

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SGC 0946 的评论

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SGC 0946 实验方案

以下实验方案包含使用 SGC 0946（目录编号 4541）的更多信息。