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Submit ReviewOICR 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.
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.
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.
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 27.78 | 50 |
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 |
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
引用文献是使用了 Tocris 产品的出版物。 OICR 9429 的部分引用包括:
Wolfgang et al (2020) Chemical Genetics Screen Identifies Epigenetic Mechanisms Involved in Dopaminergic and Noradrenergic Neurogenesis in Zebrafish. Front Genet 11 80 PMID: 32158467
Ying et al (2023) Rewired m6A epitranscriptomic networks link mutant p53 to neoplastic transformation. Nat Commun 14 1694 PMID: 36973285
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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。
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