3-(4-Pyridyl)indole
(Synonyms: Rho Kinase Inhibitor III,ROCK Inhibitor III,Rockout) 目录号 : GC12314A ROCK1 and ROCK2 inhibitor
Cas No.:7272-84-6
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
3-(4-pyridyl)indole (Rockout) is a Rho-kinase inhibitor [1].
Rho-associated protein kinase (ROCK) belongs to a family of serine-threonine kinases mainly involved in regulating the shape and movement of cells by acting on the cytoskeleton [2].
Rockout caused decreased migration and aberrant morphology. Rockout showed no effect on phagocytosis, listeria motility or actin polymerization in permeabilized yeast. In a human melanoma cell line M2 cells that blebs constitutively in a manner that is sensitive to actin cytoskeletal perturbation, Rockout (50 μM) stopped the cell blebbing within 2 min and with washout blebbing returned to normal levels within 3 min. The IC50 of Rockout was 12 μM and it inhibited blebbing in nearly all cells at 50 μM. In B3T3 cells, treatment with 50 μM Rockout resulted in significant morphological change within 10 min [1]. At an ATP concentration of 100 μM, Rockout inhibited ROCK activity with an approximate IC50 of 25 μM. Rockout (25 μM) inhibited ROCK-II and PRK to a similar degree, and MSK-1 and PKA to a lesser extent. Rockout showed no inhibitory effect on PKCα or SAPK2a [1].
References:
[1] Yarrow J C, Totsukawa G, Charras G T, et al. Screening for cell migration inhibitors via automated microscopy reveals a Rho-kinase inhibitor[J]. Chemistry & biology, 2005, 12(3): 385-395.
[2] Amano M, Fukata Y, Kaibuchi K. Regulation and functions of Rho-associated kinase[J]. Experimental cell research, 2000, 261(1): 44-51.
| Cas No. | 7272-84-6 | SDF | |
| 别名 | Rho Kinase Inhibitor III,ROCK Inhibitor III,Rockout | ||
| 化学名 | 3-(4-pyridinyl)-1H-indole | ||
| Canonical SMILES | C12=CC=CC=C1NC=C2C3=CC=NC=C3 | ||
| 分子式 | C13H10N2 | 分子量 | 194.2 |
| 溶解度 | ≤30mg/ml in ethanol;20mg/ml in DMSO;30mg/ml in dimethyl formamide | 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 | 5.1493 mL | 25.7467 mL | 51.4933 mL |
| 5 mM | 1.0299 mL | 5.1493 mL | 10.2987 mL |
| 10 mM | 0.5149 mL | 2.5747 mL | 5.1493 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。