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OICR-9429
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
OICR-9429图片
CAS NO:1801787-56-3
包装与价格：
包装价格(元)
5mg询价
25mg询价

OICR-9429 是高亲和力 WD 重复结构域 5 (WDR5) 抑制剂，通过结合 WDR5 的中央肽结合口袋竞争性阻断 WDR5 与 MLL 蛋白的相互作用。 OICR-9429 可抑制组蛋白 H3K4 三甲基化，可用于各种癌症的研究，包括非 MLL 重排白血病、结肠癌、胰腺癌、前列腺癌和膀胱癌 (BCa)。
Cas No.1801787-56-3
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 SMILESO=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℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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.

 
 
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