ML324
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-.
- 1. Qi Zhu, Feng Liang, et al. "KDM4A regulates myogenesis by demethylating H3K9me3 of myogenic regulatory factors." Cell Death Dis. 2021 May 19;12(6):514. PMID:34011940
- 2. 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
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 349.43 |
| Cas No. | 1222800-79-4 |
| Formula | C21H23N3O2 |
| Solubility | insoluble in H2O; ≥17.45 mg/mL in DMSO; ≥2.4 mg/mL in EtOH with ultrasonic |
| Chemical Name | N-(3-(dimethylamino)propyl)-4-(8-hydroxyquinolin-6-yl)benzamide |
| SDF | Download SDF |
| Canonical SMILES | CN(CCCNC(C1=CC=C(C2=CC(O)=C3C(C=CC=N3)=C2)C=C1)=O)C |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
|
Cell lines |
HFF cells |
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Preparation method |
The solubility of this compound in DMSO is > 17.5 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
|
Reacting condition |
5 ~ 50 μM |
|
Applications |
Compared with DMOG (IC50 = 0.75 mM), ML324 potently reduced IE gene expression, with an IC50 value of 10 μM. Besides, ML324 did not affect the expression of the cellular controls Sp1, S15 and TBP. In HFF cells infected with HSV-1, ML324 lowered viral yields in a dose-dependent manner (~ 4 ~ 5 logs at 25 μM) while 1.5 mM of DMOG was required to cause the same reduction. |
| Animal experiment [1]: | |
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Animal models |
A mouse ganglia explant model of latently infected mice |
|
Dosage form |
50 μM; 48 hrs |
|
Applications |
In a mouse ganglia explant model of latently infected mice, ML324 significantly inhibited viral activity. At the concentration of 50 μM, ML324 reduced the viral yield by 4.5 logs for each ganglia. Immunofluorescent staining of explanted ganglia sections showed that ML324 inhibited viral reactivation events. However, the withdrawal of ML324 resulted in marked viral replication. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
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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Quality Control & MSDS
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Chemical structure
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Related Biological Data
