UNC 0631
目录号 : GC12548
An inhibitor of G9a/GLP methyltransferases
Cas No.:1320288-19-4
Sample solution is provided at 25 µL, 10mM.
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UNC 0631 is a potent inhibitor of Protein lysine methyltransferase G9a (also known as KMT1C or EHMT2) with the IC50 value of 4nM [1].
UNC 0631 has been revealed to inhibit the G9a in SAHH-coupled with the IC50 of 4nM. Besides, UNC 0631 has been found to be highly potent in reducing H3K9me2 levels in MDA-MB-231 cells with the ICW IC50 of 25nM. In addition, UNC 0631 has been shown the high in vitro potency against G9a and improved lipophilicity. Besides, UNC 0631 has also been reported to have low cell toxicity in MDA-MB-231 cells with the IC50 value of 2.8μM in MTT assay. In different cell lines, UNC 0631 has been demonstrated to potently reduce H3K9me2 levels with the ICW IC50 of 25nM, 18nM, 26nM, 24nM, 51nM, 72nM and 46nM in MDA-MB-231, MCF7, PC3, 22RV1, HCT116 wt, HCT 116 p53 and IMR90 cell lines, respectively [1].
References:
[1] Liu F1, Barsyte-Lovejoy D, Allali-Hassani A, He Y, Herold JM, Chen X, Yates CM, Frye SV, Brown PJ, Huang J, Vedadi M, Arrowsmith CH, Jin J.Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J Med Chem. 2011 Sep 8;54( 17):6139-50.
| Cell experiment [1]: | |
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Cell lines |
MDA-MB-231 cells |
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Preparation method |
The solubility of this compound in DMSO is >18.35mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
48 h |
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Applications |
In MDA-MB-231 cells, UNC 0631 was highly potent in reducing H3K9me2 levels with IC50 value of 0.026 μM and had low cell toxicity with excellent tox/function ratios. UNC 0631 had high in vitro potency versus G9a and improved lipophilicity. UNC 0631 was valuable alternative tool compound that might be more suitable for investigating specific cellular systems. |
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References: [1] Liu F1, Barsyte-Lovejoy D, Allali-Hassani A, He Y, Herold JM, Chen X, Yates CM, Frye SV, Brown PJ, Huang J, Vedadi M, Arrowsmith CH, Jin J.Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J Med Chem. 2011 Sep 8;54( 17):6139-50. | |
| Cas No. | 1320288-19-4 | SDF | |
| 化学名 | N-(1-(cyclohexylmethyl)piperidin-4-yl)-2-(4-isopropyl-1,4-diazepan-1-yl)-6-methoxy-7-(3-(piperidin-1-yl)propoxy)quinazolin-4-amine | ||
| Canonical SMILES | COC1=C(OCCCN2CCCCC2)C=C3C(C(NC4CCN(CC5CCCCC5)CC4)=NC(N6CCN(C(C)C)CCC6)=N3)=C1 | ||
| 分子式 | C37H61N7O2 | 分子量 | 635.93 |
| 溶解度 | ≥ 18.35mg/mL in DMSO with gentle warming | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.5725 mL | 7.8625 mL | 15.725 mL |
| 5 mM | 0.3145 mL | 1.5725 mL | 3.145 mL |
| 10 mM | 0.1573 mL | 0.7863 mL | 1.5725 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: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet