IM-12
(Synonyms: GSK3β Inhibitor XIX) 目录号 : GC16617
A GSK3β inhibitor
Cas No.:1129669-05-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Kinase experiment: | Cells are lysed in RIPA buffer, supplemented with protease and phosphatase inhibitors and centrifuged for 5 min at 15,000 rpm. Immunoprecipitation of GSK-3β is performed with a specific mouse monoclonal anti GSK-3β [G8] antibody with 5 μg/sample for 2 h at 4°C. The bound protein is precipitated with Protein A/G-Plus agarose-beads (10 μL beads per sample). GSK-3β kinase activity is measured in a reaction mixture containing final concentrations of: 4 mM MOPS pH 7.2; 0.4 mM EDTA; 1 mM EGTA; 2.5 mM β-glycerophosphate; 4 mM MgCl2; 40 μM BSA; 0.05 mM DTT. 10 μg/sample pGS-2 peptide substrate is used[1]. |
Cell experiment: | To measure viable cells, 50-100 μL of cell suspension is analyzed using CASY technology with the appropriate program. ReNcell VM cells are seeded at a defined cell number and proliferated for 24 h. Then the medium is changed to proliferation medium with added substances at indicated concentrations. The cell number is determined every 24 h. Cells are exposed to the added drugs during the whole experiment, whereas the media is changed every 24 h[1]. |
References: [1]. Schmole AC, et al. Novel indolylmaleimide acts as GSK-3beta inhibitor in human neural progenitor cells. Bioorg Med Chem. 2010 Sep 15;18(18):6785-95. | |
IM-12 is a potent inhibitor of GSK-3β with IC50 value of 53 nM [1].
Glycogen synthase kinase-3β (GSK-3β) is a proline-directed serine-threonine kinase and is involved in neuronal cell development, energy metabolism and body pattern formation. Inhibition of GSK-3β can cause β-catenin accumulation.
IM-12 is a potent GSK-3β inhibitor. In ReNcell VM cells, IM-12 significantly increased total β-catenin by 27% and at a concentration of 3 µM increased the β-catenin amount most. In ReNcell VM cells, IM-12 (3 µM) inhibited GSK-3β to a remaining activity of 27 ± 5%. Also, IM-12 significantly increased the cell doubling time to 26.5 ± 0.9 h and significantly inhibited cell proliferation. In ST14A cells, IM-12 caused an accumulation of β-catenin around the nucleus. In ReNcell VM cells transfected with TOPFlash, IM-12 increased TCF-activity. In cells transfected with TOP and pCAGGS-S33Y (a vector containing β-catenin), IM-12 significantly increased TCF-activity by 270%. In ReNcell VM cells, IM-12 significantly increased the level of βIIItub+ cells to 3.7 ± 0.7%, which suggested that IM-12 increased neuronal differentiation [1].
Reference:
[1]. Schmöle AC, Brennführer A, Karapetyan G, et al. Novel indolylmaleimide acts as GSK-3beta inhibitor in human neural progenitor cells. Bioorg Med Chem, 2010, 18(18): 6785-6795.
| Cas No. | 1129669-05-1 | SDF | |
| 别名 | GSK3β Inhibitor XIX | ||
| Canonical SMILES | FC1=CC=C(C=C1)CCNC2=C(C(N(C)C2=O)=O)C3=C(C)NC4=CC=CC=C34 | ||
| 分子式 | C22H20FN3O2 | 分子量 | 377.41 |
| 溶解度 | ≥ 18.85mg/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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6496 mL | 13.2482 mL | 26.4964 mL |
| 5 mM | 0.5299 mL | 2.6496 mL | 5.2993 mL |
| 10 mM | 0.265 mL | 1.3248 mL | 2.6496 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。