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Y-27632

现货
Catalog No.
B1293
ROCK选择性抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 500.00
Ship with 10-15 days
10mg
¥ 800.00
Ship with 10-15 days
50mg
¥ 3,200.00
Ship with 10-15 days
200mg
¥ 8,800.00
Ship with 10-15 days

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Background

Y-27632 is a specific inhibitor of Rho-associated kinases(ROCK) family with Ki values of 0.22μM and 0.30μM for ROCK1 and ROCK2, respectively.

Y-27632 has shown selectivity of inhibition by comparing their Ki values for other Rho effector kinases, citron kinase and PKN, as well as PKCα. The Ki values of Y-27632 for citron kinase and PKN are least 20-fold higher, and Ki values for PKCα are about 200-fold higher than those for ROCK kinases. In addition, Y-27632 has been reported to inhibit ROCK1 and ROCK2 by competing with ATP for binding to the kinase in HeLa cells. Besides, Y-27632 has also shown the inhibition of stress fibers in Swiss 3T3 cells when the concentration of Y-27632 is 10μM [1].

References:
[1] Ishizaki T1, Uehata M, Tamechika I, Keel J, Nonomura K, Maekawa M, Narumiya S. Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases. Mol Pharmacol. 2000 May;57(5):976-83.

文献引用

1. Zhou N, Lee JJ, et al. "Rho Kinase Regulates Aortic Vascular Smooth Muscle Cell Stiffness Via Actin/SRF/Myocardin in Hypertension." Cell Physiol Biochem. 2017 Nov 23;44(2):701-715. PMID:29169155
2. Pazhoohan S, Raoufy MR, et al. "Effect of Rho-kinase inhibition on complexity of breathing pattern in a guinea pig model of asthma." PLoS One. 2017 Oct 31;12(10):e0187249. PMID:29088265
3. GUANGQI ZHOU, XINMEI LIU, et al. "Homeobox B4 inhibits breast cancer cell migration by directly binding to StAR-related lipid transfer domain protein 13." ONCOLOGY LETTERS,August 3, 2017.
4. Wang E, Wang D, et al. "Growth of hollow cell spheroids in microbead templated chambers." Biomaterials. 2017 Oct;143:57-64. PMID:28763630
5. Jones BC, Kelley LC, et al. "Dual Targeting of Mesenchymal and Amoeboid Motility Hinders Metastatic Behavior." Mol Cancer Res. 2017 Jun;15(6):670-682. PMID:28235899
6. Lamborn IT, Jing H, et al. "Recurrent rhinovirus infections in a child with inherited MDA5 deficiency." J Exp Med. 2017 Jul 3;214(7):1949-1972. PMID:28606988
7. Wang Y, Gunasekara DB, et al. "A microengineered collagen scaffold for generating a polarized crypt-villus architecture of human small intestinal epithelium." Biomaterials. 2017 Jun;128:44-55. PMID:28288348
8. Jones BC, Kelley LC, et al. "Dual Targeting of Mesenchymal and Amoeboid Motility Hinders Metastatic Behavior." Mol Cancer Res. 2017 Feb 24. PMID:28235899
9. Chan W, Akhbanbetova A, et al. "Topical delivery of a Rho-kinase inhibitor to the cornea via mucoadhesive film." Eur J Pharm Sci. 2016 May 16. PMID:27196964

Chemical Properties

StorageStore at -20°C
M.Wt247.34
Cas No.146986-50-7
FormulaC14H21N3O
Solubility≥24.7mg/mL in DMSO, <1mg/mL in Chloroform
Chemical Name4-[(1R)-1-aminoethyl]-N-pyridin-4-ylcyclohexane-1-carboxamide
SDFDownload SDF
Canonical SMILESCC(C1CCC(CC1)C(=O)NC2=CC=NC=C2)N
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。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。

试验操作

激酶实验 [1]:

激酶实验

通过使用Lipofectamine在HeLa细胞中转染Myc标记的重组ROCK-1、ROCK-II、PKN或citron激酶,并通过使用9E10单克隆抗Myc抗体偶联G蛋白琼脂糖凝胶从细胞裂解物中进行沉淀。在不存在或存在各种浓度的Y-27632下,将回收的免疫复合物与各种浓度的[32P]ATP及10 mg组蛋白2作为底物一起温育,于总体积为30 ml激酶缓冲液中30℃反应30分钟,缓冲液包含50 mM HEPES-NaOH、pH 7.4、10 mM MgCl2、5 mM MnCl2、0.02%Briji 35和2 mM二硫苏糖醇。在不存在或存在各种浓度的Y-27632下,将PKCa与5 mM [32P] ATP和200 mg/ml组蛋白2作为底物,在30℃下在总体积为30 ml的激酶缓冲液中反应30 min,缓冲液配方为50 mM Tris-HCl、pH 7.5、0.5 mM CaCl2,5 mM乙酸镁,25 mg/ml磷脂酰丝氨酸,50 ng/ml 12-O-tetradecanoylphorbol-13-acetate和0.001%亮肽素。使用43 Laemmli样品缓冲液(10 ml)终止反应。

细胞实验 [1]:

细胞系

HeLa细胞,Swiss 3T3细胞

溶解方法

该化合物在DMSO中的溶解度大于10 mM。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月

反应条件

0.3和1 μM, 30 min或24 h

应用

Y-27632抑制ROCK-1和ROCK-II的激酶活性,ATP以竞争性方式逆转了这种抑制作用。在Swiss 3T3细胞中,Y-27632(10 μM)消除了应激纤维,但在该浓度下,细胞周期的G1-S转变和胞质分裂几乎不受影响。在Swiss 3T3细胞中,Y-27632细胞预处理30分钟以浓度依赖性方式防止细胞形状及肌动蛋白应激纤维发生变化,在10 μM浓度下几乎完全抑制。10和100 μM的Y-27632延长了延迟时间,并以浓度依赖性方式将BrdU标记细胞的出现延迟约1和4小时。在HeLa细胞中,30 μM Y-27632抑制胞质分裂。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

References:

[1]. Ishizaki T, Uehata M, Tamechika I, et al. Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases[J]. Molecular pharmacology, 2000, 57(5): 976-983.

生物活性

描述 Y-27632是ROCK1(p160ROCK)的选择性抑制剂,Ki值为140 nM。
靶点 ROCK1 (p160ROCK) ROCK2        
IC50 140 nM(Ki) 300 nM(Ki)        

质量控制

化学结构

Y-27632

相关生物数据

Y-27632

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Y-27632

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Y-27632

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Y-27632

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Y-27632

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Y-27632

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Y-27632