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My CartCAS：129830-38-2
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 129830-38-2 |
| Name | Y-27632 dihydrochloride |
| Molecular Formula | C14H21N3O·2HCl |
| Molecular Weight | 320.26 |
| Solubility | Soluble in Water/DMSO ≥5mg/mL |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 813-428-5 |
| MDL | MFCD03490488 |
| SMILES | O=C([C@@H]1CC[C@]([C@H](N)C)([H])CC1)NC2=CC=NC=C2.[H]Cl.[H]Cl |
| Target Point | ROCK |
| Passage | Cytoskeleton; Cell Cycle;TGF-beta/Smad;Stem Cells |
| Background | Y-27632 dihydrochloride is an ATP-competitive ROCK-I and ROCK-II inhibitor. |
| Biological Activity | Y-27632 dihydrochloride 是 ATP 竞争性的 ROCK-I 和 ROCK-II 抑制剂，Ki 分别为 220 nM 和 300 nM。[1-4] |
| In Vitro | Y-27632抑制ROCK家族的激酶比其他激酶(包括蛋白激酶C，cAMP依赖性激酶和肌球蛋白轻链激酶)强100倍。 Y-27632延长滞后时间并以浓度依赖性方式延迟BrdU标记细胞的出现，在分别用10和100μMY-27632处理的Swiss 3T3细胞中观察到约1和4小时的延迟[1] ]。 Y-27632促进脂肪组织来源的干细胞(ADSCs)的神经元分化。与1.0和2.5μMY-27632诱导组相比，神经样细胞的百分比在5.0μMY-27632诱导组中达到峰值[2]。 |
| In Vivo | 与盐水组相比，Y-27632(5和10 mg/kg)显著延长肌阵挛性抽搐的起效时间。与生理盐水组相比，Y-27632(5和10 mg/kg)显著延长阵挛性惊厥的发作时间[3]。与对照动物(SS组)相比，用二甲基亚硝胺(DMN)治疗导致大鼠体重和肝脏重量(DMN-S组)显著降低。口服Y27632(30 mg/kg)基本上可以防止这种DMN诱导的大鼠体重和肝脏重量减轻(DMN-Y组)[4]。 |
| Cell Experiment | HeLa细胞以每3.5cm培养皿3×104个细胞的密度接种。在10mM胸苷存在下，将细胞在含有10％FBS的DMEM中培养16小时。用含有10％FBS的DMEM洗涤细胞后，再培养8小时，然后加入40ng/mL的诺考达唑。在Nocodazole处理11.5小时后，加入各种浓度的Y-27632(0-300μM)，Y-30141或载体，并将细胞再孵育30分钟[1]。 |
| Animal Experiment | 小鼠[3]使用体重25-30g的雄性近交瑞士白化小鼠(2-3个月大)。每周给小鼠注射亚痉挛剂量的PTZ(35mg/kg，ip)(周一，周三和周五)，共注射11次。在每次PTZ注射后，观察小鼠30分钟并记录惊厥活动的发生。 30分钟后，然后给小鼠注射法舒地尔(25mg/kg，ip)或Y-27632(5mg/kg，ip)并返回其家笼，直至下一次注射。用于法舒地尔和Y-27632的对照小鼠接受盐水。大鼠[4]雄性Wistar种A大鼠(200-250g)。将DMN(1μg/ mL)用盐水(终浓度1％)稀释10倍，并且在每周的前3天腹膜内(ip)注射10mg/kg每天的DMN，持续4周。从第一次注射DMN开始，每天以30mg/kg的剂量口服给予Y27632，持续4周。 30mg/kg的剂量在几种大鼠模型中校正高血压而没有毒性。将20只大鼠随机分成4个实验组(每组n = 5)，如下：(1)SS(腹腔注射生理盐水和口服生理盐水);(2)SY(腹腔注射生理盐水和口服Y27632);(3)DMN-S(DMN ip和口服盐水);(4)DMN-Y(DMN ip和口服Y27632)。每周称重大鼠。在第四周结束时将它们处死并切除肝脏。另外，在处死大鼠之前立即采集血样。 |
| Kinase Experiment | 通过使用Lipofectamine转染，重组ROCK-1，ROCK-II，PKN或citron激酶在HeLa细胞中表达为Myc标记的蛋白，并通过使用与G蛋白偶联的9E10单克隆抗Myc抗体从细胞裂解物中沉淀。 - 琼脂糖。回收的免疫复合物与不同浓度的[32P] ATP和10mg组蛋白2型作为底物在不存在或存在各种浓度的Y-27632或Y-30141的条件下于30℃温育30分钟，总体积为30μL含有50mM HEPES-NaOH，pH 7.4，10mM MgCl 2，5mM MnCl 2，0.02％Briji 35和2mM二硫苏糖醇的激酶缓冲液。将PKCa与5μM[32P] ATP和200μg/ mL组蛋白2型作为底物孵育，在不存在或存在各种浓度的Y-27632或Y-30141的情况下，在含有50μL的激酶缓冲液中于30°C保持10分钟mM Tris-HCl，pH 7.5，0.5mM CaCl 2，5mM乙酸镁，25μg/ mL磷脂酰丝氨酸，50ng/mL 12-O-十四烷基佛波醇-13-乙酸酯和0.001％亮抑酶肽，总体积为30μL。通过添加10μL的43 Laemmli样品缓冲液终止孵育。煮沸5分钟后，将混合物在16％凝胶上进行SDS-聚丙烯酰胺凝胶电泳。用考马斯亮蓝染色凝胶，然后干燥。切除对应于组蛋白2型的条带，并测量放射性[1]。 |
| Data Literature Source | [1]. Ishizaki T，et al. Pharmacological properties of Y-27632，a specific inhibitor of rho-associated kinases. Mol Pharmacol. 2000 May;57(5):976-83. [2]. Xue ZW，et al. Rho-associated coiled kinase inhibitor Y-27632 promotes neuronal-like differentiation of adult human adipose tissue-derived stem cells.Chin Med J (Engl). 2012 Sep;125(18):3332-5. [3]. Inan S，et al. Antiepileptic effects of two Rho-kinase inhibitors，Y-27632 and fasudil，in mice. Br J Pharmacol. 2008 Sep;155(1):44-51. [4]. Tada S，et al. A selective ROCK inhibitor，Y27632，prevents dimethylnitrosamine-induced hepatic fibrosis in rats. J Hepatol. 2001 Apr;34(4):529-36. |
| Unit | Bottle |
| Specification | 5mg 10mg 50mg |
In the process of class organs culture, generally without Y - 27632. Y-27632 is a potent and selective small molecule inhibitor of ROCK1(p160ROCK), capable of targeting catalytic sites that bind ROCK-1 and ROCK-2, thereby inhibiting their kinase activity. Y-27632, which is commonly used in organoid construction, can significantly inhibit the apoptosis of stem cells caused by dissociation and improve the efficiency of clone formation, and is one of the indispensable components in the stem cell culture process.
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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