ML324 (Synonyms: CID-44143209) |
カタログ番号GC12557 |
ML324 は、抗ウイルス活性を持つ強力な JMJD2 デメチラーゼ阻害剤です。 ML324 は、ヒストン脱メチル化酵素 KDM4B の阻害も示し、IC50 は 4.9 μM です。 ML324 は、ウイルスの IE 遺伝子発現を阻害することにより、単純ヘルペス ウイルス (HSV) とヒト サイトメガロ ウイルス (hCMV) の両方の感染に対して強力な抗ウイルス活性を示します。
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Cas No.: 1222800-79-4
Sample solution is provided at 25 µL, 10mM.
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-.
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