LOM612
目录号 : GC32921
LOM612是一种有效的FOXO核移位激活剂，在细胞中EC50值为1.5μM。
Cas No.:2173232-79-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | Cells are seeded at a concentration of 1× 104 cells/well in 200 μL culture medium and incubated at 37°C in 5% CO2. After 24 hours, when the monolayer formed, the medium is replaced with a final volume of 200 μL of new medium with tested compounds (LOM612, etc.) or controls are added to the plates. Cells are treated with eight 2-fold serial dilutions of each compound spanning concentrations from 50 μM to 0.39 μM in 1% DMSO final. Controls are on the first and the last columns of the plates. On the first column, methyl methanesulfonate (MMS) acts as a positive control and DMSO as a negative control. When compounds (LOM612, etc.) and controls are added, plates are incubated at 37°C in 5% CO2 incubator for 72 hours. After this time, MTT solution is prepared at 5 mg/mL in PBS 1X and then diluted at 0.5 mg/mL in MEM without phenol red. The sample solution in wells is flicked off and 100 μL of MTT dye is added to each well. The plates are gently shaken and incubated for 3 hours at 37°C in 5% CO2 incubator. The supernatant is removed and 100 μL of DMSO 100% is added. The plates are gently shaken to solubilize the formed formazan. The absorbance is measured at a wavelength of 570 nm[1]. |
References: [1]. Cautain B, et al. Discovery of a Novel, Isothiazolonaphthoquinone-Based Small Molecule Activator of FOXO Nuclear-Cytoplasmic Shuttling. PLoS One. 2016 Dec 9;11(12):e0167491. | |
LOM612 is a potent activator of FOXO nuclear translocation, with an EC50 value of 1.5 μM in cells.
LOM612 potently activates nuclear translocation of FOXO with an EC50 value of 1.5 μM, and this effect is independent of CRM-1. LOM612 effectively induces translocation of endogenous FOXO3a and FOXO1, and increases the expression of the FOXO target genes p27 and FasL. LOM612 shows no effect on the nuclear export of endogenous NFKB2 transcription factor in U2OS cells. LOM612 is cytotoxic to HepG2 cells, with an IC50 value of 0.64 μM, and does not sensitize non-cancer THLE2 cells (IC50, 2.76 μM)[1].
[1]. Cautain B, et al. Discovery of a Novel, Isothiazolonaphthoquinone-Based Small Molecule Activator of FOXO Nuclear-Cytoplasmic Shuttling. PLoS One. 2016 Dec 9;11(12):e0167491.
| Cas No. | 2173232-79-4 | SDF | |
| Canonical SMILES | O=C1C2=C(SN=C2N(C)C)C(C3=CC=CC=C31)=O | ||
| 分子式 | C13H10N2O2S | 分子量 | 258.3 |
| 溶解度 | DMSO : 6 mg/mL (23.23 mM);Water : < 0.1 mg/mL (insoluble) | 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 | 3.8715 mL | 19.3573 mL | 38.7147 mL |
| 5 mM | 0.7743 mL | 3.8715 mL | 7.7429 mL |
| 10 mM | 0.3871 mL | 1.9357 mL | 3.8715 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。
Discovery of a Novel, Isothiazolonaphthoquinone-Based Small Molecule Activator of FOXO Nuclear-Cytoplasmic Shuttling
PLoS One 2016 Dec 9;11(12):e0167491.PMID:27936162DOI:PMC5147912
FOXO factors are tumour suppressor proteins commonly inactivated in human tumours by posttranslational modifications. Furthermore, genetic variation within the FOXO3a gene is consistently associated with human longevity. Therefore, the pharmacological activation of FOXO proteins is considered as an attractive therapeutic approach to treat cancer and age-related diseases. In order to identify agents capable of activating FOXOs, we tested a collection of small chemical compounds using image-based high content screening technology. Here, we report the discovery of LOM612 (compound 1a), a newly synthesized isothiazolonaphthoquinone as a potent FOXO relocator. Compound 1a induces nuclear translocation of a FOXO3a reporter protein as well as endogenous FOXO3a and FOXO1 in U2OS cells in a dose-dependent manner. This activity does not affect the subcellular localization of other cellular proteins including NFkB or inhibit CRM1-mediated nuclear export. Furthermore, compound 1a shows a potent antiproliferative effect in human cancer cell lines.