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ML324

现货
Catalog No.
B4891
JMJD2去甲基化酶抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 600.00
现货
10mg
¥ 680.00
现货
50mg
¥ 2,220.00
Ship with 10-15 days
200mg
¥ 5,930.00
Ship with 10-15 days

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Background

ML324 is a potent and cell-permeable JMJD2 demethylase inhibitor (IC50 = 920 nM). [1]
Jumonji-domain-containing proteins (JMJD) is the largest class of N ε -methyl lysine demethylase, an enzyme that demethylates the tri-methylated H3K9. JMJD takes part in gene transcription regulation. [1]
ML324 acted as an antiviral agent that effectively inhibited HSV and hCMV IE gene expression in HFF and MRC-5 cells, resulted in suppression of HSV plaques formation and inhibition of HSV infection spread. [1]
ML324 also blocked HSV-1 reactivation and inhibited the formation of HSV plaque in mouse ganglia explant model of latently infected mice. [1]
References:
1.Rai G, Kawamura A, Tumber A, Liang Y, Vogel JL, Arbuckle JH, Rose NR,
Dexheimer TS, Foley TL, King ON, Quinn A, Mott BT, Schofield CJ, Oppermann U,Jadhav A, Simeonov A, Kristie TM, Maloney DJ. Discovery of ML324, a JMJD2
demethylase inhibitor with demonstrated antiviral activity. 2012 Dec 17 [updated 2013 Sep 16]. Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.

文献引用

1. Li N, Yang L, et al. "BET bromodomain inhibitor JQ1 preferentially suppresses EBV-positive nasopharyngeal carcinoma cells partially through repressing c-Myc." Cell Death Dis. 2018 Jul 9;9(7):761. PMID:29988031

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt349.43
Cas No.1222800-79-4
FormulaC21H23N3O2
Solubility≥17.45mg/mL in DMSO
Chemical NameN-(3-(dimethylamino)propyl)-4-(8-hydroxyquinolin-6-yl)benzamide
SDFDownload SDF
Canonical SMILESCN(CCCNC(C1=CC=C(C2=CC(O)=C3C(C=CC=N3)=C2)C=C1)=O)C
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

HFF细胞

制备方法

在DMSO中的溶解度大于17.5 mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

5 ~ 50 μM

实验结果

与DMOG (IC50 = 0.75 mM) 相比,ML324有效下调IE基因表达,其IC50值为10 μM。此外,ML324不影响对照Sp1、S15和TBP的表达。在感染了HSV-1的HFF细胞中,ML324呈剂量依赖性地减少病毒产量(在25 μM的剂量下,病毒产量减少了约4-5 logs)。对于DMOG,达到等同效果需要其浓度达到1.5 mM。

动物实验 [1]:

动物模型

小鼠神经节外植体模型的潜在感染小鼠

给药剂量

50 μM;48小时

实验结果

在小鼠神经节外植体模型的潜在感染小鼠中,ML324显著抑制病毒活性。在50 μM的浓度下,ML324使每个神经节的病毒产量降低了4.5个对数。外植神经节切片的免疫荧光染色显示,ML324抑制病毒重新激活。然而,撤回ML324导致病毒复制显著。

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. Rai G, Kawamura A, Tumber A, Liang Y, Vogel JL, Arbuckle JH, Rose NR, Dexheimer TS, Foley TL, King ON, Quinn A, Mott BT, Schofield CJ, Oppermann U,Jadhav A, Simeonov A, Kristie TM, Maloney DJ. Discovery of ML324, a JMJD2 demethylase inhibitor with demonstrated antiviral activity. 2012 Dec 17 [updated 2013 Sep 16]. Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.

质量控制

化学结构

ML324

Related Biological Data

ML324