OICR 9429

Pricing Availability   Qty
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)
说明书
引用文献 (2)
评论
文献 (2)

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.

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
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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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:

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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