ML324
(Synonyms: CID-44143209) 目录号 : GC12557
A cell-permeable inhibitor of JMJD2 demethylases
Cas No.:1222800-79-4
Sample solution is provided at 25 µL, 10mM.
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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-.
| Cell experiment [1]: | |
|
Cell lines |
HFF cells |
|
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]: | |
|
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. |
|
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-. | |
| Cas No. | 1222800-79-4 | SDF | |
| 别名 | CID-44143209 | ||
| 化学名 | N-(3-(dimethylamino)propyl)-4-(8-hydroxyquinolin-6-yl)benzamide | ||
| Canonical SMILES | CN(CCCNC(C1=CC=C(C2=CC(O)=C3C(C=CC=N3)=C2)C=C1)=O)C | ||
| 分子式 | C21H23N3O2 | 分子量 | 349.43 |
| 溶解度 | ≥ 17.45mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.8618 mL | 14.309 mL | 28.618 mL |
| 5 mM | 0.5724 mL | 2.8618 mL | 5.7236 mL |
| 10 mM | 0.2862 mL | 1.4309 mL | 2.8618 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet