DIM-C-pPhCO2Me
目录号 : GC34557
DIM-C-pPhCO2Me是一种核受体4A1（NR4A1）拮抗剂，Ki值为0.25µM。
Cas No.:151358-48-4
Sample solution is provided at 25 µL, 10mM.
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DIM-C-pPhCO2Me is a nuclear receptor 4A1 (NR4A1) antagonist, with a Ki value of 0.25µM [1]. DIM-C-pPhCO2Me can inhibit the migration of cancer cells by inhibiting the activity of NR4A1 and increasing the mRNA and protein expression of IL24[2]. DIM-C-pPhCO2Me has been widely used to inhibit the growth of different cancer cells and induce apoptosis[3].
In vitro, DIM-C-pPhCO2Me treatment for 24 hours significantly inhibited the proliferation of ACHN cells and 786-O cells with IC50 values of 11.7μM and 13.4μM, respectively[4]. Treatment with 20µM DIM-C-pPhCO2Me for 48h inhibited Rh30 cell growth and decreased the expression of survivin, bcl-2, cyclin D1, EGFR, and cMyc in cells[5]. Treatment of 20µM DIM-C-pPhCO2Me for 24h reduced β1-integrin and α5-integrin expression in SW480 cells and inhibited cell adhesion and migration[6].
In vivo, DIM-C-pPhCO2Me treatment via gavage at a dose of 40mg/kg (every other day for 20 days) inhibited tumor growth in athymic nude mice bearing Rh30 cells as xenografts[5]. A single dose of 2mg/kg DIM-C-pPhCO2Me administered intratracheally 30min before E. coli infection significantly increased mouse survival and global protein levels in bronchoalveolar lavage fluid[7].
References:
[1] Lee S O, Li X, Hedrick E, et al. Diindolylmethane analogs bind NR4A1 and are NR4A1 antagonists in colon cancer cells[J]. Molecular endocrinology, 2014, 28(10): 1729-1739.
[2] Lacey A, Hedrick E, Cheng Y, et al. Interleukin-24 (IL24) is suppressed by PAX3-FOXO1 and is a novel therapy for rhabdomyosarcoma[J]. Molecular cancer therapeutics, 2018, 17(12): 2756-2766.
[3] Wu L, Chen L. Characteristics of Nur77 and its ligands as potential anticancer compounds[J]. Molecular medicine reports, 2018, 18(6): 4793-4801.
[4] Hedrick E, Lee S O, Kim G, et al. Nuclear receptor 4A1 (NR4A1) as a drug target for renal cell adenocarcinoma[J]. PloS one, 2015, 10(6): e0128308.
[5] Lacey A, Hedrick E, Li X, et al. Nuclear receptor 4A1 (NR4A1) as a drug target for treating rhabdomyosarcoma (RMS)[J]. Oncotarget, 2016, 7(21): 31257.
[6] Hedrick E, Lee S, Safe S. The nuclear orphan receptor NR4A1 regulates β1‐integrin expression in pancreatic and colon cancer cells and can be targeted by NR4A1 antagonists[J]. Molecular carcinogenesis, 2017, 56(9): 2066-2075.
[7] Cui P, Wu S, Xu X, et al. Deficiency of the transcription factor NR4A1 enhances bacterial clearance and prevents lung injury during Escherichia coli pneumonia[J]. Shock, 2019, 51(6): 787-794.
DIM-C-pPhCO2Me是一种核受体4A1（NR4A1）拮抗剂，Ki值为0.25µM[1]。DIM-C-pPhCO2Me能通过抑制NR4A1活性并增加IL24的mRNA和蛋白表达来抑制癌细胞的迁移[2]。DIM-C-pPhCO2Me已被广泛用于抑制不同癌细胞的生长并诱导细胞凋亡[3]。
在体外，DIM-C-pPhCO2Me 处理24小时显著抑制了ACHN细胞和786-O细胞的增殖，IC50值分别为11.7µM和13.4µM[4]。使用20µM的DIM-C-pPhCO2Me 处理48小时，抑制了Rh30细胞的生长，并降低了细胞中survivin、bcl-2、cyclin D1、EGFR和cMyc的表达[5]。使用20µM的DIM-C-pPhCO2Me处理24小时，降低了SW480细胞中β1-整合素和α5-整合素的表达，并抑制了细胞粘附和迁移[6]。
在体内，以40mg/kg的剂量通过灌胃给予DIM-C-pPhCO2Me（每隔一天一次，持续20天），抑制了携带Rh30细胞异种移植瘤的无胸腺裸鼠的肿瘤生长[5]。在大肠杆菌感染前30分钟，单次气管内给予2mg/kg剂量的DIM-C-pPhCO2Me，显著提高了小鼠的存活率，并增加了支气管肺泡灌洗液中的总蛋白水平[7]。
| Cell experiment [1]: | |
Cell lines | 786-O cells |
Preparation Method | 786-O cells were cultured in Dulbecco’s modified Eagle’s medium/Ham’s F-12 or RPMI-1460 medium medium supplemented with 10% fetal bovine serum and 1% antibiotics at 37°C in the presence of 5% CO2. 786-O cells were seeded in 12-well plates at a density of 1.0×105 cells/well and cultured for 24 hours to make adherent cells. After incubation for 24 hours, the cells were treated with different concentrations of DIM-C-pPhCO2Me (7.5, 15, and 20µM) for 24 hours, and DMSO was used as a control. Subsequently, cells were digested with trypsin at the indicated time points, and cell counts were performed. |
Reaction Conditions | 7.5, 15, and 20µM; 24h |
Applications | DIM-C-pPhCO2Me treatment decreased the cell viability of 786-O cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Female athymic nude mice |
Preparation Method | Female athymic nude mice (6-8 weeks of age) were maintained under specific pathogen clearance (SPF) conditions. Rh30 cells (4×106 cells) cultured in RPMI medium containing 10% fetal bovine serum (FBS) were digested, resuspended in 100μl of Matrigel containing phosphate buffer (PBS) (75:25), and subcutaneously implanted into mice. When the tumor volume reached about 40-50mm3, the mice were randomly divided into control group and treatment group (n = 6 each), and were given a placebo or DIM-C-pPhCO2Me (40mg/kg) by gavage every other day for 20 days. Tumor volume, weight, and body weight of mice were determined. |
Dosage form | 40mg/kg; every other day for 20 days; p.o. |
Applications | DIM-C-pPhCO2Me treatment significantly suppressed tumor growth in athymic nude mice bearing Rh30 cells as xenografts. |
References: | |
| Cas No. | 151358-48-4 | SDF | |
| Canonical SMILES | COC(C1=CC=C(C(C2=CNC3=C2C=CC=C3)C4=CNC5=C4C=CC=C5)C=C1)=O | ||
| 分子式 | C25H20N2O2 | 分子量 | 380.44 |
| 溶解度 | DMSO : ≥ 125 mg/mL (328.57 mM) | 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 | 2.6285 mL | 13.1427 mL | 26.2854 mL |
| 5 mM | 525.7 μL | 2.6285 mL | 5.2571 mL |
| 10 mM | 262.9 μL | 1.3143 mL | 2.6285 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
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- Purity: >99.50%
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