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Submit ReviewWDR5 0103 is a WD repeat-containing protein 5 (WDR5) antagonist (Kd = 450 nM). Disrupts WDR5 interaction with MLL and inhibits MLL core complex methyltransferase activity in vitro. Has no effect on a panel of seven other methyltransferases, including SETD7.
WDR5 0103 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。
分子量 | 383.44 |
公式 | C21H25N3O4 |
储存 | Store at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 890190-22-4 |
PubChem ID | 6457069 |
InChI Key | ZPLBXOVTSNRBFB-UHFFFAOYSA-N |
Smiles | O=C(OC)C1=CC(NC(C3=CC=CC(OC)=C3)=O)=C(N2CCN(C)CC2)C=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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 38.34 | 100 | |
ethanol | 19.17 | 50 |
以下数据基于产品分子量 383.44。 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 | 2.61 mL | 13.04 mL | 26.08 mL |
5 mM | 0.52 mL | 2.61 mL | 5.22 mL |
10 mM | 0.26 mL | 1.3 mL | 2.61 mL |
50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
参考文献是支持产品生物活性的出版物。
Senisterra et al (2013) Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5. Biochem.J. 449 151 PMID: 22989411
If you know of a relevant reference for WDR5 0103, please let us know.
关键词: WDR5 0103, WDR5 0103 supplier, WDR50103, WDR5, antagonists, MLL, methyltransferases, epigenetics, WD, repeat-containing, WD40, Lysine, Methyltransferases, 5323, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。
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Reaction mixtures with various concentrations of WDR5-0103 (1 μM–1 mM) were incubated for 1 h at room temperature and then quenched by adding 20 μL of 7.5 M guanidinium chloride.
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。
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.
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.