DDO-2093

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

DDO-2093 

DDO-2093 是一种有效的 MLL1 和 WDR5 蛋白-蛋白相互作用抑制剂 (IC50=8.6 nM; Kd= 11.6 nM)，具有抗肿瘤活性。DDO-2093 选择性抑制 MLL 复合物的催化活性。

DDO-2093

DDO-2093 Chemical Structure

CAS No. : 2250024-74-7

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生物活性

DDO-2093 is a potent MLL1-WDR5 protein-protein interaction inhibitor (IC50=8.6 nM; Kd=11.6 nM) with antitumor activity. DDO-2093 selectively inhibits the catalytic activity of MLL complex[1].

体外研究
(In Vitro)

DDO-2093 (5 μM; pretreated 7 days) inhibits MLL-fusion protein dependent genes expression (HOXA9 and Meis1)[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 1, 2.5, 5, and 10 μM
Incubation Time: Pretreated 7 days
Result: Dose-dependently reduced the mono-, di-, and trimethylation of H3K4.

体内研究
(In Vivo)

DDO-2093 (20 mg/kg-80 mg/kg; i.p.; every other day for 21 days) significantly suppresses the tumor size and weight in a dose-dependent manner[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female nude mice (MV4-11 human leukemia cancer xenografts)[1]
Dosage: 20 mg/kg, 40 mg/kg and 80 mg/kg
Administration: I.p.; every other day for 21 days
Result: The tumor volume growth inhibition (GI) values were calculated to be 13.7%, 37.6% and 63.9% with doses of 20 mg/kg, 40 mg/kg and 80 mg/kg, respectively.

分子量

614.11

Formula

C29H37ClFN9O3
CAS 号

2250024-74-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Chen W, et al. Discovery of a potent MLL1 and WDR5 protein-protein interaction inhibitor with in vivo antitumor activity [published online ahead of print, 2021 Jun 28]. Eur J Med Chem. 2021;223:113677.

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