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OICR-9429 Sale

目录号 : GC16397

A probe for WDR5

OICR-9429 Chemical Structure

Cas No.:1801787-56-3

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5mg
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25mg
¥2,070.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

IC50: 5 uM

OICR-9429 is an antagonist of Wdr5-MLL interaction.

WDR5 has been identified as a component of the MLL complex, which is required for histone H3 tri-methylation by its binding of histone H3. Thus, WDR5 is reported to be a presenter component of MLL, suggesting that WDR5 can bind substrates of methylated histone H3 to the MLL complex for further methylation.

In vitro: Previous study found that Wdr5 could be detected readily in C/EBPα immunoprecipitates from lysates of Cebpap30/p30 cells by the treatment of OICR-9429, indicating that the Wdr5-MLL interaction could not influence p30 binding. Moreover, the gene expression profiling of OICR-9429-treated Cebpap30/p30 cells showed that Wdr5 antagonism could result in the upregulation of myeloid-specific transcripts. In addition, the gene set enrichment analyses demonstrated a close correlation between OICR-9429–induced genes and genes that were upregulated after Wdr5 knockdown. Furthermore, the gene profile of Cebpap30/p30 LICs6 was downregulated due to the Wdr5 antagonism caused by OICR-9429. Further treatment of OICR-9429 to Cebpap30/p30 cells was found to be associated with myeloid differentiation and loss of progenitor morphology [1].

In vivo: So far, there is no animal in vivo data reported.

Clinical trial: Up to now, OICR-9429 is still in the preclinical development stage.

Reference:
[1] Grebien F et al.  Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia. Nat Chem Biol.2015 Aug;11(8):571-8.

Chemical Properties

Cas No. 1801787-56-3 SDF
化学名 N-(4-(4-methylpiperazin-1-yl)-3'-(morpholinomethyl)-[1,1'-biphenyl]-3-yl)-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide
Canonical SMILES O=C(C(C(C(F)(F)F)=C1)=CNC1=O)NC2=CC(C3=CC=CC(CN4CCOCC4)=C3)=CC=C2N5CCN(C)CC5
分子式 C29H32F3N5O3 分子量 555.59
溶解度 DMSO: 0.5 mg/ml (with gentle warming),Methanol: 0.5 mg/ml (with gentle warming) 储存条件 Store at -20°C
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1 mM 1.7999 mL 8.9994 mL 17.9989 mL
5 mM 0.36 mL 1.7999 mL 3.5998 mL
10 mM 0.18 mL 0.8999 mL 1.7999 mL
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