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CAS No.: 1222800-79-4

ML324 Catalog No. CSN13837

Synonyms: CID-44143209

ML324 is an inhibitor of JMJD2 demethylase with IC50 of 920 nM with antiviral activity.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 JMJD2

IC50:920nM
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]
动物研究
剂量
Mice: 0.2 mg/kg^[2] (i.v.); 60 mg/kg^[3] (i.p.)

给药途径
i.v., i.p.
参考文献

动物研究
剂量	Mice: 0.2 mg/kg^[2] (i.v.); 60 mg/kg^[3] (i.p.)
给药途径	i.v., i.p.

[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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8618 mL
- 14.3092 mL
- 28.6183 mL
- 5 mM
- 0.5724 mL
- 2.8618 mL
- 5.7237 mL
- 10 mM
- 0.2862 mL
- 1.4309 mL
- 2.8618 mL

技术信息

CAS号

1222800-79-4

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H23N3O2

运输

蓝冰

分子量

349.43

别名

CID-44143209

溶解度

DMSO	26.0 mg/mL (74.4 mM) warming
Water	Insoluble
Ethanol	6.0 mg/mL (17.2 mM) warming

动物实验配方

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