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Submit ReviewOICR 9429
说明： High affinity and selective WDR5 antagonist
化学名： N-[2-(4-Methylpiperazin-1-yl)-5-[3-(morpholin-4-ylmethyl)phenyl]phenyl]-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide
纯度： ≥98% (HPLC)
生物活性 for OICR 9429
OICR 9429 is a high affinity WDR5 antagonist (Kd = 93 nM; IC50 = 64 nM); disrupts WDR5-MLL interaction. Exhibits selectivity for WDR5 over 22 methyltransferases and a panel of kinases, GPCRs, ion channels, and transporters. Reduces viability of acute myeloid leukemia cells in vitro. Also disrupts MLL1-RbBP5 interaction.
To request the negative control for OICR 9429, please fill out the OICR 0547 request form on the SGC website.
许可信息
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the OICR-9429 probe summary on the SGC website.
External Portal Information for OICR 9429
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of OICR 9429 is reviewed on the chemical probes website.
技术数据 for OICR 9429
| 分子量 | 555.59 |
| 公式 | C29H32F3N5O3 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1801787-56-3 |
| PubChem ID | 91623360 |
| InChI Key | DJOVLOYCGXNVPI-UHFFFAOYSA-N |
| Smiles | CN(CC4)CCN4C1=C(NC(C5=CNC(C=C5C(F)(F)F)=O)=O)C=C(C2=CC(CN3CCOCC3)=CC=C2)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.
溶解性数据 for OICR 9429
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 27.78 | 50 |
制备储备液 for OICR 9429
以下数据基于产品分子量 555.59。 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 |
|---|---|---|---|
| 0.5 mM | 3.6 mL | 18 mL | 36 mL |
| 2.5 mM | 0.72 mL | 3.6 mL | 7.2 mL |
| 5 mM | 0.36 mL | 1.8 mL | 3.6 mL |
| 25 mM | 0.07 mL | 0.36 mL | 0.72 mL |
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产品说明书 for OICR 9429
参考文献 for OICR 9429
参考文献是支持产品生物活性的出版物。
Grebien et al (2015) Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia. Nat.Chem.Biol. 11 571 PMID: 26167872
Getlik et al (2016) Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1). J.Med.Chem. 59 2478 PMID: 26958703
If you know of a relevant reference for OICR 9429, please let us know.
关键词: OICR 9429, OICR 9429 supplier, OICR9429, High, affinity, selective, WDR5, antagonists, WD, repeat-containing, proteins, 5, antagonism, sgc, WD40, Lysine, Methyltransferases, 5267, Tocris Bioscience
2 篇 OICR 9429 的引用文献
引用文献是使用了 Tocris 产品的出版物。 OICR 9429 的部分引用包括：
Ying et al (2023) Rewired m6A epitranscriptomic networks link mutant p53 to neoplastic transformation. Nat Commun 14 1694 PMID: 36973285
Wolfgang et al (2020) Chemical Genetics Screen Identifies Epigenetic Mechanisms Involved in Dopaminergic and Noradrenergic Neurogenesis in Zebrafish. Front Genet 11 80 PMID: 32158467
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