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Y-27632 dihydrochloride

目录号 M1817 所有产品仅供科研使用，严禁用于人或动物的治疗等任何其他用途，不为任何个人提供产品和服务  

Y-27632 2HCl是一种选择性的ROCK1(p160ROCK)抑制剂，Ki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。此外，Y-27632能与Thiazovivin提高重编程效率，促进iPSCs的产生。

Y-27632 dihydrochloride结构式

别名：Y27632; Y-27632 2HCl

规格 价格 库存状态
Free Sample (0.5-1 mg)  ¥ 0 中国库存现货
10mM*1mL in DMSO ¥ 900 中国库存现货
2mg ¥ 450 中国库存现货
5mg ¥ 630 中国库存现货
10mg ¥ 900 中国库存现货
50mg ¥ 2880 中国库存现货
其他规格数量报价？
质量标准及产品资料
生物活性

Y-27632 2HCl是一种选择性的ROCK1(p160ROCK)抑制剂，Ki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。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。此外，Y-27632能与Thiazovivin提高重编程效率，促进iPSCs的产生。

使用AbMole产品发表的文献
产品使用成果展示
数据来源 Cancer Discov (2018 Sep). Figure 1. Y27632 (AbMole BioScience)
方法 general culture
细胞系/动物模型 Pleural effusion fluid
浓度 10 uM
处理时间
实验结果 Illustration of organoid generation from tumor, to plating in Matrigel, to organoid growth
数据来源 Advanced materials (2018 Oct). Figure 1. Y-27632 (Abmole Bioscience)
方法 Organoid Isolation and Culturing
细胞系/动物模型 Mouse small intestinal organoids
浓度 10 × 10−6 M
处理时间 20-45 min
实验结果 The frequency of cyst formation from single intestinal stem cells after three days (colony formation efficiency) was equally high in the fibrin gel supplemented with 10% v/v BME as in pure BME.
数据来源 Nature Microbiology (2018). Figure 3. Y27632 (AbMole BioScience)
方法 cell culture
细胞系/动物模型 Lung tissue
浓度 10 uM
处理时间 2 weeks
实验结果 Lastly, IFA of sporozoiteinfected organoids using Crypt-a-Glo showed newly formed oocysts at six days post infection
数据来源 Oncotarget (2017). Figure 6. Y27632 (Abmole Bioscience)
方法 intraperitoneally
细胞系/动物模型 SCID mice
浓度 25 mg/kg
处理时间 18 days
实验结果 Similar to our in vitro findings, Y27632 significantly increased the expression of PAI-1, confirming the existence of a regulatory mechanism between ROCK and PAI-1 in vivo
数据来源 Oncotarget (2017). Figure 5. Y27632 (Abmole Bioscience)
方法 intraperitoneally
细胞系/动物模型 SCID mice
浓度 25 mg/kg
处理时间 18 days
实验结果 After 18 days of treatment, we did not observe any effect of PQ401, Y27632 or PQ401 combined with Y27632 on primary tumor growth, suggesting that the inhibition of ROCK or IGF-1 receptor did not affect cancer cell proliferation.
数据来源 Oncotarget (2017). Figure 4. Y27632 (Abmole Bioscience)
方法 immunoblotting
细胞系/动物模型 MDA-MB-231 cell
浓度 10 μM
处理时间 72 h
实验结果 Interestingly, PAI-1 expression increased in cells treated with Y27632, suggesting the existence of a regulatory loop between PAI-1 and ROCK
数据来源 Oncotarget (2017). Figure 2. Y27632 (Abmole Bioscience)
方法 Transwell
细胞系/动物模型 MDA-MB-231 cells
浓度 10 μM
处理时间 72 h
实验结果 Y27632 did not affect the scattering and invasion of MDA-MB-231 cultured without CAFs, but significantly reduced the scattering and invasion induced by CAFs, suggesting that CAFs promote the invasion of MDA-MB-231 cells via ROCK1/2.
数据来源 Nat Protoc (2018). Figure 1. Y-27632 (Abmole Bioscience)
方法 i.e.
细胞系/动物模型 NSG (NOD.Cg-Prkd cscidIl 2rgtm1Wjl/SzJ) mice
浓度 10 μM
处理时间 5–10 min
实验结果 Administration of tamoxifen to these mice induces specific activation of the Cre enzyme within the epithelial cells of the small and large intestine, with consequential deletion of both Apc alleles, expression of an oncogenic form of Kras (KrasG12D) and deletion of one of the two Trp53 alleles
数据来源 University of California (2017). Figure 7. Y-27632 (Abmole Bioscience)
方法 Patient-derived organoid culture
细胞系/动物模型 biopsy tissue
浓度 10 μM
处理时间 30 min
实验结果 mCRPC patient-derived organoids are sensitive to olaparib. Organoids from patients with homozygous loss of CHD1 (V5272 and V5372) show increased sensitivity to PARP inhibition.
数据来源 Nat Protoc (2018). Figure 4. Y-27632 dihydrochloride (Abmole Bioscience, USA)
方法 FACS plots
细胞系/动物模型 Human liver single-cell
浓度 10 μM
处理时间 7 d
实验结果 FACS plots depicting gating strategies for sorting single cells from a human liver organoid culture
数据来源 Cell (2017). Figure 1. Y-27632 (Abmole Bioscience)
方法 PARPi assay
细胞系/动物模型 BC organoid lines
浓度 < 100 μm
处理时间 48 h
实验结果 Inhibition of Rho-associated coiled-coil containing protein kinase (ROCK) has been shown to allow long-term proliferation of tumor epithelial cells in vitro and addition of the specific ROCK inhibitor Y-27632 indeed improved culture conditions.
数据来源 Am J Clin Exp Urol (2017) . Figure 1. Y-27632 (Abmole Bioscience, USA)
方法 Organoid culture
细胞系/动物模型 LNCaP and C4-2B cells
浓度 10 μM
处理时间 48-72 h
实验结果 A few cells presented as an aggregate of two cells or three cells. At day 7, LNCaP cells and C4-2B cells started to present aggregates of multiple cells. At day 14, organoids were formed as aggregates of LNCaP cells and C4-2B cells
数据来源 Nature Protocols (2016) . Figure 3. Y-27632 (Abmole Bioscience)
方法 MTT assay
细胞系/动物模型 mouse and human luminal cell
浓度 10 μM
处理时间 2–3 d
实验结果 Absence of the ROCK inhibitor (Y-27632) will greatly decrease the efficiency of organoid outgrowth.
数据来源 Nature (2016). Figure 1. Y-27632 (Abmole Bioscience Inc)
方法 Cell culture.
细胞系/动物模型 single cells
浓度 10 μM
处理时间
实验结果
数据来源 Materials Science and Engineering (2017). Figure 8. Y-27632 (Abmole Bioscience Inc, USA)
方法 Cytoskeleton and nucleus staining in the absence or presence of ROCK inhibitor (Y-27632)
细胞系/动物模型 SaOS-2 cells
浓度 10 μM
处理时间 4 h and 24 h
实验结果 After inhibition of ROCK by Y-27632, an expected formation of finger-like filopodia was seen for the cells of all groups after 4 h, as shown by white arrows in Fig. 8b, f and j.
数据来源 Materials Science and Engineering (2017). Figure 7. Y-27632 (Abmole Bioscience Inc, USA)
方法 Cytoskeleton and nucleus staining in the absence or presence of ROCK inhibitor (Y-27632)
细胞系/动物模型 SaOS-2 cells
浓度 10 μM
处理时间 4 h and 24 h
实验结果 The attached cells on the three investigated surfaces in the presence or absence (control) of Y-27632 after 4 h and 24 h were summarized in Fig. 7
实验参考
体外实验*
细胞系 cyES cells
方法 For 5-bromo-2′-deoxyuridine (BrdU) incorporation assays, dissociated cyES cells were seeded at a concentration of 500 cells/cm2 onto fresh feeder layers in the presence of the ROCK inhibitors Y-27632 (Wako Pure Chemical Industries, Tokyo, Japan) or Fasudil (Tocris Bioscience, MO, USA) during the first 24 h of culture. The BrdU incorporation assay was performed using colorimetric BrdU Cell proliferation Kit (Roche Diagnostics) according to the manufacturer's instructions. BrdU incorporations were also observed by immunocytochemical (ICC) staining with BrdU Labeling and Detection Kit I (Roche Diagnostics).
浓度 0, 0.1, 0.5, 5, 10, 20µM
处理时间 24 h

*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

体内实验*
动物模型 EAC modeling
配制 dissolved in 0.9% NaCl
剂量 0.1, 1, 10 mg/kg/day for 14 days
给药处理 i.p.

*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

化学性质
分子量 320.26
分子式 C14H21N3O.2HCl
CAS号 129830-38-2
溶解性（25°C） Water ≥ 60 mg/mL
DMSO ≥ 45 mg/mL
储存条件 粉末型式       -20°C   3年；4°C   2年
溶于溶剂       -80°C   6个月；-20°C   1个月
运输方式 冰袋运输，根据产品的不同，可能会有相应调整。
储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.1225 mL 15.6123 mL 31.2246 mL
5 mM 0.6245 mL 3.1225 mL 6.2449 mL
10 mM 0.3122 mL 1.5612 mL 3.1225 mL
不同实验动物依据体表面积的等效剂量转换表（参考来源于公开文献）
小鼠 大鼠 兔 豚鼠 仓鼠 狗
重量 (kg) 0.02 0.15 1.8 0.4 0.08 10
体表面积 (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km 系数 3 6 12 8 5 20
动物 A (mg/kg) = 动物 B (mg/kg) ×  动物 B的Km系数
动物 A的Km系数

例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

参考文献

[1] Li X, et al. Stem Cells Dev. The ROCK inhibitor Y-27632 enhances the survival rate of human embryonic stem cells following cryopreservation.

[2] Honjo M, et al. Invest Ophthalmol Vis Sci. Effects of rho-associated protein kinase inhibitor Y-27632 on intraocular pressure and outflow facility.

[3] Ishizaki T, et al. Mol Pharmacol. Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases.

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