Y-27632 2HCl
Y-27632 2HCl是一种选择性ROCK1和ROCK2抑制剂，无细胞试验中Ki分别为140 nM和300nM，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。
Y-27632 2HCl Chemical Structure
CAS: 129830-38-2
产品质控
常与Y-27632 2HCl一起在实验中被使用的化合物
Y-27632 2HCl和SB202190，与其他抑制剂一起，使人原代真皮成纤维细胞中生成诱导性间充质干细胞(iMSCs)。
Y-27632 2HCl和SB431542联合可逆转mTEC-KO小鼠细胞中TGF-β1诱导的间充质肌动蛋白细胞骨架应激纤维。
Y-27632 2HCl和CHIR99021共同降低野生型(WT)和PKP2mut心肌细胞中脂肪生成基因的表达。
Y-27632 2HCl可减少MG132预处理后MYLA细胞中由TNFα引起的P-IκBα多聚泛素化。
Y27632 2HCl和Z-VAD-FMK可阻断H2O2诱导的PC12细胞膜起泡和胞核凝聚。
Y-27632 2HCl相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| SW620 | Growth Inhibition Assay | 10 μM | 18 d | Does not inhibit cell growth | 10021386 |
| HCT15 | Growth Inhibition Assay | 10 μM | 18 d | Does not inhibit cell growth | 10021386 |
| HCT116 | Growth Inhibition Assay | 10 μM | 18 d | Strongly inhibits cell growth | 10021386 |
| LS174T | Growth Inhibition Assay | 10 μM | 18 d | Moderately inhibits cell growth | 10021386 |
| Neonatal rat ventricular myocytes | Function Assay | 10 μM | 48 h | Inhibits ET-1-induced increases in protein synthesis, cell size and myofibrillar organization | 10386613 |
| Stellate Cell | Function Assay | 25 μM | 15 min | Inhibits formation of F-actin stress fibers and phosphorylation of myosin light chain | 10600496 |
| Rat Vascular Smooth Muscle Cells | Function Assay | 10 μM | 2 h | Inhibits angiotensin II-induced hypertrophy | 10642317 |
| PC3 | Function Assay | 25 μM | 1 h | Induces morphological changes | 10720471 |
| PC3 | Migration Assay | 25 μM | 1 h | Inhibits the BMFB-CM and the EGF-stimulated migration | 10720471 |
| PC3 | Growth Inhibition Assay | 25 μM | 17 h | Does not inhibit cell growth | 10720471 |
| LNCaP | Growth Inhibition Assay | 25 μM | 17 h | Does not inhibit cell growth | 10720471 |
| Rat hepatic stellate cells | Function Assay | 30 μM | 48 h | Diminishes the phosphorylation of Erk2, and decreases new DNA synthesis | 10845663 |
| Pancreatic acinar cells | Function Assay | 10 μM | 70 min | Potentiates CCK-stimulated pancreatic enzyme secretion | 12745080 |
| C2C12 | Function Assay | 10 μM | 6 h | Prevents the serine phosphorylation of IRS-1 induced by insulin and/or TNF-α | 16267124 |
| PC 12 | Function Assay | 10 μM | 24 h | Attenuates catecholamine biosynthesis | 16219424 |
| Cynomolgus monkey embryonic stem cells | Cytotoxic Assay | 20 µM | 24 h | Promotes cyES cell survival | 18940855 |
| TSGH 8301 | Migration Assay | 20 µM | 1 h | Increases cell migration | 19896475 |
| Swiss3T3 | Colony-forming Assay | 10 µM | 13 d | Increases prostate cell colony-forming activity | 21464902 |
| HT22 | Cytotoxic Assay | 10 µM | 13 h | Protects against glutamate-induced neuronal death | 22810835 |
| Salivary gland stem cells | Function Assay | 10 µM | 7 d | Reduces SGSC senescence | 25804560 |
| Src-2 | Growth Inhibition Assay | 10 μM | 18 d | Does not inhibit cell growth | 10021386 |
| Src-1 | Growth Inhibition Assay | 10 μM | 18 d | Does not inhibit cell growth | 10021386 |
| NIH3T3 | Growth Inhibition Assay | 10 μM | 18 d | Does not inhibit cell growth | 10021386 |
| Src-4 | Growth Inhibition Assay | 10 μM | 18 d | Does not inhibit cell growth | 10021386 |
| Src-1 | Growth Inhibition Assay | 10 μM | 18 d | Does not inhibit cell growth | 10021386 |
| Ras-4 | Growth Inhibition Assay | 10 μM | 18 d | Strongly inhibits cell growth | 10021386 |
| Ras-2 | Growth Inhibition Assay | 10 μM | 18 d | Strongly inhibits cell growth | 10021386 |
| mNET1-e | Growth Inhibition Assay | 10 μM | 18 d | Strongly inhibits cell growth | 10021386 |
| mNET1-d | Growth Inhibition Assay | 10 μM | 18 d | Strongly inhibits cell growth | 10021386 |
| Dbl-e | Growth Inhibition Assay | 10 μM | 18 d | Moderately inhibits cell growth | 10021386 |
| Dbl-d | Growth Inhibition Assay | 10 μM | 18 d | Strongly inhibits cell growth | 10021386 |
| NIH3T3 | Growth Inhibition Assay | 10 μM | 18 d | Does not inhibit cell growth | 10021386 |
| Mesothelial cells from rat mesentery | Invasive Assay | 30 μM | 20 h | Blocks invasive activity | 9930872 |
| CCL39 | Function Assay | 30 μM | 30 min | Completely abolishes activation of Na-H exchanger NHE1 by integrins | 9693382 |
| HeLa | Function Assay | 10 μM | 30 min | Inhibits the formation of stress fibers and the assembly of vinculin-containing focal adhesions | 9668072 |
| N1E-115 | Function Assay | 10 μM | 2 h | Inhibits the assembly of microtubules and intermediate filaments to form extended processes | 9647654 |
| Swiss 3T3 cells | Function Assay | 10 μM | 2 h | Inhibits the assembly of microtubules and intermediate filaments to form extended processes | 9647654 |
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Y-27632 2HCl是一种选择性ROCK1和ROCK2抑制剂，无细胞试验中Ki分别为140 nM和300nM，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 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Y-27632也同等有效抑制ROCK-II。Y-27632作用于PKC, cAMP依赖的蛋白激酶和 肌球蛋白轻链激酶(MLCK)几乎没有活性，Ki分别为26 μM, 25 μM, 和 > 250 μM。Y-27632通过选择性抑制Ca2+敏感化，而抑制多种兴奋剂而不是KCl，包括Phenylephrine, Histamine, Acetylcholine, Serotonin, Endothelin,和Thromboxane诱导的平滑肌收缩，IC50为0.3-1 μM。Y-27632 作用于培养的细胞，抑制Rho诱导的, p160ROCK调节的应力纤维的形成。[1] Y-27632处理，阻断 Rho调节的肌动球蛋白的激活，也阻断LPA刺激的MM1 细胞入侵活性，这种作用存在浓度依赖性。[2] 10 μM Y-27632 处理在无血清悬浮(SFEB)培养基中的人类胚胎干细胞(hES)，显著减少分离诱导的凋亡，提高克隆效率(从~1%提高到~27%), 转基因后促进亚克隆,且使SFEB培养的hES细胞存活及分化成Bf1+皮质和基底端脑祖细胞。[5] |
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|---|---|---|---|---|
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western Blot | p-LIMK1(Thr508) p-LIMK2(Thr505) p-Cofilin(Ser3) CDK2 KRT7 ROCK2 E-cadherin p-MLC2(Ser19) |
|
24704720 | |
| Transwell migration assay | cell migration inhibition |
|
27694793 | |
| Immunofluorescence | Neurotoxicity Assay E-cadherin beta-catenin Phalloidin |
|
21362567 | |
| Growth inhibition assay | cell proliferation |
|
24523903 | |
| ELISA | caspase-9 |
|
30320378 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | Y-27632按30 mg/kg剂量口服处理自发性高血压大鼠，肾性高血压大鼠，及去氧皮质酮醋酸(DOCA)盐高血压大鼠，显著降低血压，这种作用存在剂量依赖性。[1] Y-27632按每小时0.55 μL通过植入泵持续处理表达Val14-RhoA的大鼠，持续11天，延迟 MM1 细胞入侵。[2] Y-27632作用于肺循环，通过抑制ROCK, 降低 缺氧诱导的血管生成，和血管重构。[4] |
|
|---|---|---|
| 动物实验 | Animal Models | 携带自发或诱发高血压的雄性Wistar大鼠; 艾利希腹水癌小鼠模型 |
| Dosages | 30 mg/kg/day (大鼠)；0-10 mg/kg （小鼠） | |
| Administration | 口服处理 (大鼠)；ip（小鼠） | |
化学信息&溶解度
| 分子量 | 320.26 | 分子式 | C14H21N3O.2HCl |
| CAS号 | 129830-38-2 | SDF | Download Y-27632 2HCl SDF |
| Smiles | CC(C1CCC(CC1)C(=O)NC2=CC=NC=C2)N.Cl.Cl | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 64 mg/mL ( (199.83 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : 64 mg/mL (199.83 mM) Ethanol : 4 mg/mL (12.48 mM) |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
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）
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Selleck为您提供正确的澄清溶液配方）
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，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
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 ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：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。
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常见问题及建议解决方法
问题 1:
Is there any data about the Amax (maximum attraction luminosity) and extinction coefficient of this compound?
回答：
The wavelength we used to test HPLC is 260nm while the extinction coefficient is unknown.
问题 2:
Could this product be used in cell culture? Do you have any reference for this application?
回答：
Yes. The Y-27632 can be used in cell culture certainly. Here is the reference website: http://molpharm.aspetjournals.org/content/57/5/976.full.
