Y-27632 dihydrochloride
Catalog No.
A3008
ROCK1抑制剂
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Y-27632 dihydrochloride是一种Rho相关蛋白激酶p160ROCK的小分子抑制剂，IC50值为140 nM。Y-27632靶向结合ROCK-1和ROCK-2的催化位点，从而抑制它们的激酶活性。因此，Y-27632可以作用于Rho介导的应力纤维的形成，抑制G1-S期细胞周期进程和胞质分裂。
参考文献：
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| Physical Appearance | A solid |
| Storage | Desiccate at 4°C or below |
| M.Wt | 320.26 |
| Cas No. | 129830-38-2 |
| Formula | C14H21N3O·2HCl |
| Synonyms | y-27632, Y27632, Y-27632 dihydrochloride, Y 27632 |
| Solubility | ≥111.2 mg/mL in DMSO; ≥17.57 mg/mL in EtOH; ≥52.9 mg/mL in H2O |
| Chemical Name | 4-[(1R)-1-aminoethyl]-N-pyridin-4-ylcyclohexane-1-carboxamide |
| SDF | Download SDF |
| Canonical SMILES | CC(C1CCC(CC1)C(=O)NC2=CC=NC=C2)N |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验[1]： | |
|
细胞系 |
人（hu）和大鼠（r）前列腺平滑肌细胞（PSM） |
|
溶解方法 |
在DMSO中的溶解度>10 mM。为了获得更高的浓度，可以将离心管在37°C加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20°C以下储存几个月。 |
|
反应条件 |
100 μM；24 h和48 h |
|
应用 |
在表达Rho激酶的前列腺平滑肌细胞中研究Rho激酶抑制剂Y-27632是否会影响细胞活力和增殖。huPSM和rPSM在无血清培养基中静置24小时，在缺乏或存在Y-27632（0.01-100 μM）时，用1%血清刺激后的24小时和48小时用中性红和MTT实验评估细胞活力。实验结果表明，1%血清再刺激后的24小时和48小时孵育期之间细胞数量增加。而在Y-27632存在时，活细胞数量的增加少于对照组，该效果是浓度依赖的。 |
| 动物实验[2]： | |
|
动物模型 |
成年雄性Swiss白化小鼠 |
|
剂量 |
0.1 mg/kg/day；腹腔注射 |
|
应用 |
组织病理学检查表明，EAC荷瘤小鼠用Y-27632治疗后减少了60-70%的病理结构，向正常的完整组织结构变化，尤其是在癌前治疗中。Y-27632对ROCK的抑制显著减少肿瘤的迁移和侵袭。免疫组化结果显示，在癌前而非癌后治疗组，ROCK2主要被Y-27632抑制。 |
|
注意事项 |
请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的，属于正常现象。 |
|
References: [1] Rees R W, Foxwell N A, Ralph D J, et al. Y-27632, a Rho-kinase inhibitor, inhibits proliferation and adrenergic contraction of prostatic smooth muscle cells[J]. The Journal of urology, 2003, 170(6): 2517-2522. [2] Isler D, Ozaslan M, Karagoz I D, et al. Antitumoral effect of a selective Rho-kinase inhibitor Y-27632 against Ehrlich ascites carcinoma in mice[J]. Pharmacological Reports, 2014, 66(1): 114-120. |
|
| 描述 | Y-27632是一种选择性的ROCK1 (p160ROCK)抑制剂，Ki值为140 nM。比对其他激酶包括PKC、cAMP依赖性蛋白激酶、MLCK和PAK的作用强200多倍。 | |||||
| 靶点 | ROCK1 | ROCK2 | ||||
| IC50 | 140 nM (Ki) | 300 nM (Ki) | ||||
质量控制和MSDS
- 批次:
化学结构
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