ML324

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Chemical Structure| 1222800-79-4 同义名 : CID-44143209
CAS号 : 1222800-79-4
货号 : A214803
分子式 : C21H23N3O2
纯度 : 99%+
分子量 : 349.426
MDL号 : MFCD28053518
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(85.86 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • KDM4

    JMJD2, IC50:920 nM
描述 ML324 is the first potent and cell permeable JMJD2E inhibitor with IC50 value of 920nM. In contrast to previously reported inhibitors of the JMJD proteins, ML324 displays excellent cell permeability. It demonstrated potent anti-viral activity against both herpes simplex virus (HSV) and human cytomegalovirus (hCMV) infection via inhibition viral IE gene expression at 50μM. ML324 suppressed the formation of HSV plaques, even at high MOI, and blocked HSV-1 reactivation in a mouse ganglia explant model of latently infected mice[4].
作用机制 ML324 may chelate the active site iron.[4]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.86mL

0.57mL

0.29mL

14.31mL

2.86mL

1.43mL

28.62mL

5.72mL

2.86mL
参考文献

[1]Rai G, Kawamura A, et al. Discovery of ML324, a JMJD2 demethylase inhibitor with demonstrated antiviral activity.

[2]Choi JY, Yoon SS, et al. KDM4B histone demethylase and G9a regulate expression of vascular adhesion proteins in cerebral microvessels. Sci Rep. 2017 Mar 22;7:45005.

[3]Wang W, Oguz G, et al. KDM4B-regulated unfolded protein response as a therapeutic vulnerability in PTEN-deficient breast cancer. J Exp Med. 2018 Nov 5;215(11):2833-2849.

[4]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]. In: Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010–. PMID: 24260783.