Dynole 2-24
目录号 : GC66056
Dynole 2-24 是一种基于吲哚的 dynamin GTPase 抑制剂 (对 dynamin I的IC50=0.56 μM)。Dynole 2-24 无毒，在体外和细胞内显示出增强的抗动力蛋白I和II的效力 (IC??(CME)=1.9 μM)。Dynole 2-24 对 dynamin I的选择性为4.4倍。Dynole 2-24在网格蛋白介导的内吞作用的细胞抑制剂中具有活性。CME: Clathrin mediated endocytosis
Cas No.:1416313-72-8
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
Dynole 2-24 is an indole-based dynamin GTPase inhibitor (IC50=0.56 μM for dynamin I). Dynole 2-24 is nontoxic and shows increased potency against dynamin I and II in vitro and in cells (IC??(CME)=1.9 μM). Dynole 2-24 also shows 4.4-fold selectivity for dynamin I. Dynole 2-24 is active in-cell inhibitor of clathrin-mediated endocytosis[1]. CME: Clathrin mediated endocytosis
| Cas No. | 1416313-72-8 | SDF | Download SDF |
| 分子式 | C24H41N3 | 分子量 | 371.6 |
| 溶解度 | 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 | 2.6911 mL | 13.4553 mL | 26.9107 mL |
| 5 mM | 0.5382 mL | 2.6911 mL | 5.3821 mL |
| 10 mM | 0.2691 mL | 1.3455 mL | 2.6911 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。
Synthesis of Dynole 34-2, Dynole 2-24 and Dyngo 4a for investigating dynamin GTPase
Nat Protoc 2014 Apr;9(4):851-70.PMID:24651498DOI:10.1038/nprot.2014.046.
Dynamin is a large GTPase with roles in membrane fission during clathrin-mediated endocytosis, in actin dynamics and in cytokinesis. Defects in dynamin have been linked to human diseases. The synthesis of a dynamin modulator toolkit comprising two different inhibitor classes is described. The first series comprises Dynole 34-2, Dynole 2-24 and the inactive control Dynole 31-2. The Dynole compounds act on the dynamin G domain, are not GTP competitive and can be synthesized in 2-3 d. Knoevenagel condensation of 1-(3-(dimethylamino)propyl)-1H-indole-3-carbaldehyde (1) with cyanoamides (2 and 3) affords Dynole 31-2 and Dynole 34-2, respectively. Reductive amination of 1 with decylamine gives Dynole 2-24. The second series acts at an allosteric site in the G domain of dynamin and comprises Dyngo 4a and Dyngo Ø (inactive control). Both are synthesized in an overnight reaction via condensation of 3-hydroxy-2-naphthoic hydrazide with 2,4,5-trihydroxybenzaldehyde to afford Dyngo 4a, or with benzaldehyde to afford Dyngo Ø.