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Y-27632

Y-27632

产品编号 T1870   CAS 146986-50-7

Y-27632 (Y-27632) 是一种 ROCK-I 和 ROCK-II 抑制剂,具有口服有效性、ATP 竞争性。Y-27632 还抑制分离诱导的小鼠前列腺干或祖细胞凋亡

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Y-27632 Chemical Structure
Y-27632, CAS 146986-50-7
规格 价格/CNY 折后价 货期 数量
1 mg ¥ 248 ¥ 124 现货
2 mg ¥ 355 ¥ 177 现货
5 mg ¥ 578 ¥ 289 现货
10 mg ¥ 747 ¥ 373 现货
25 mg ¥ 1,450 ¥ 725 现货
50 mg ¥ 2,660 ¥ 1,330 现货
100 mg ¥ 3,290 ¥ 1,645 现货
200 mg ¥ 4,810 ¥ 2,405 现货
1 mL * 10 mM (in DMSO) ¥ 555 ¥ 277 现货
其他形式的 Y-27632:
产品目录号及名称: Y-27632 (T1870)
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纯度: 99.87%
纯度: 99.87%
纯度: 99.83%
纯度: 99.73%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Y-27632 dihydrochloride (Y-27632 2HCl) is an orally potent, ATP-competitive inhibitor of ROCK-I and ROCK-II. Y-27632 dihydrochloride also inhibits isolation-induced apoptosis in mouse prostate stem or progenitor cells.
靶点活性 ROCKI:220 nM(ki), ROCKII:300 nM(ki)
体外活性 方法:人诱导多能干细胞 marmoset iPSC 用 Y-27632 (5-20 μM) 处理 7 天,使用 AKP 检测克隆形成情况。
结果:Y-27632 显著提高 marmoset iPSC 的克隆效率。[1]
方法:成人脂肪组织衍生干细胞 ADSCs 用 Y-27632 (5 μmol/L) 处理 1 h,检测 ADSCs 的形态变化。
结果:Y-27632 剂量依赖性诱导 ADSCs 的神经元分化,5 μmol/L Y-27632 处理 1 h 的 ADSCs的神经元样细胞百分比为(93.5±4.7)%。[2]
方法:食蟹猴胚胎干细胞 cyES 常规传代或用 Y-27632 (1-10 μM) 处理 24 h,使用 Flow Cytometry 方法进行活-死染色,使用试剂盒检测 BrdU。
结果:Y-27632 促进 cyES 存活细胞增加。Y-27632 没有促进细胞增殖,但保护细胞在单细胞消化后免于细胞死亡。[3]
体内活性 方法:为研究 Y-27632 在运动神经元疾病的治疗潜力,将 Y-27632 (2 or 30 mg/kg in drinking water) 口服给 ALS 模型的 SOD1G93A 小鼠,持续 137 天。
结果:Y-27632 2 mg/kg 治疗的效果不佳,Y-27632 30 mg/kg 治疗可改善雄性小鼠的运动功能,雌性小鼠仅表现出有限的改善。[4]
方法:为研究 Y-27632 对肝纤维化的影响,将 Y-27632 (30 mg/kg) 口服给药给 dimethylnitrosamine (DMN) 诱导肝纤维化的大鼠,每天一次,持续四周。
结果:Y-27632 治疗显著减少了 DMN 诱导的肝纤维化的发生,并降低了肝脏中胶原和羟脯氨酸的含量以及 α-SMA 的表达。[5]
激酶实验 Recombinant ROCK-I, ROCK-II, PKN, or citron kinase is expressed in HeLa cells as Myc-tagged proteins by transfection using Lipofectamine, and is precipitated from the cell lysates by the use of 9E10 monoclonal anti-Myc antibody coupled to G protein-Sepharose. Recovered immunocomplexes are incubated with various concentrations of [32P]ATP and 10 mg of histone type 2 as substrates in the absence or presence of various concentrations of either Y-27632 or Y-30141 at 30°C for 30 min in a total volume of 30 μL of the kinase buffer containing 50 mM HEPES-NaOH, pH 7.4, 10 mM MgCl2, 5 mM MnCl2, 0.02% Briji 35, and 2 mM dithiothreitol. PKCa is incubated with 5 μM [32P]ATP and 200 μg/mL histone type 2 as substrates in the absence or presence of various concentrations of either Y-27632 or Y-30141 at 30°C for 10 min in a kinase buffer containing 50 mM Tris-HCl, pH 7.5, 0.5 mM CaCl2, 5 mM magnesium acetate, 25 μg/mL phosphatidyl serine, 50 ng/mL 12-O-tetradecanoylphorbol-13-acetate and 0.001% leupeptin in a total volume of 30 μL. Incubation is terminated by the addition of 10 μL of 43 Laemmli sample buffer. After boiling for 5 min, the mixture is subjected to SDS-polyacrylamide gel electrophoresis on a 16% gel. The gel is stained with Coomassie Brilliant Blue, and then dried. The bands corresponding to histone type 2 are excised, and the radioactivity is measured[1].
细胞实验 Y-27632 is dissolved in water and stored[1]. HeLa cells are plated at a density of 3×104 cells per 3.5-cm dish. The cells are cultured in DMEM containing 10% FBS in the presence of 10 mM Thymidine for 16 h. After the cells are washed with DMEM containing 10% FBS, they are cultured for an additional 8 h, and then 40 ng/mL of Nocodazole is added. After 11.5 h of the Nocodazole treatment, various concentrations of Y-27632 (0-300 μM), Y-30141, or vehicle is added and the cells are incubated for another 30 min[1].
化合物与蛋白结合的复合物

T1870_1

The Catalytic Subunit of cAMP-dependent Protein Kinase (PKA) in Complex with Rho-kinase Inhibitor Y-27632

分子量 247.34
分子式 C14H21N3O
CAS No. 146986-50-7

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: 1 mg/ml (4.04 mM)

DMSO: 100 mM

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 4.043 mL 20.2151 mL 40.4302 mL 101.0754 mL
DMSO 5 mM 0.8086 mL 4.043 mL 8.086 mL 20.2151 mL
10 mM 0.4043 mL 2.0215 mL 4.043 mL 10.1075 mL
20 mM 0.2022 mL 1.0108 mL 2.0215 mL 5.0538 mL
50 mM 0.0809 mL 0.4043 mL 0.8086 mL 2.0215 mL
100 mM 0.0404 mL 0.2022 mL 0.4043 mL 1.0108 mL

计算器

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参考文献

1. Wu Y, et al. ROCK inhibitor Y27632 promotes proliferation and diminishes apoptosis of marmoset induced pluripotent stem cells by suppressing expression and activity of caspase 3. Theriogenology. 2016 Jan 15;85(2):302-14. 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. Takehara T, et al. Rho-associated kinase inhibitor Y-27632 promotes survival of cynomolgus monkey embryonic stem cells. Mol Hum Reprod. 2008 Nov;14(11):627-34. 4. Günther R, et al. The rho kinase inhibitor Y-27632 improves motor performance in male SOD1(G93A) mice. Front Neurosci. 2014 Oct 7;8:304. 5. Tada S, et al. A selective ROCK inhibitor, Y27632, prevents dimethylnitrosamine-induced hepatic fibrosis in rats. J Hepatol. 2001 Apr;34(4):529-36.

文献引用

1. Chen Y P, Shao Y, Chen P C, et al.Substrate nesting guides cyst morphogenesis of human pluripotent stem cells without 3D extracellular matrix overlay.Acta Biomaterialia.2023 2. Wang X, Liang X, Zhou L, et al. Yes-associated protein reacts differently in vascular smooth muscle cells under different intensities of mechanical stretch. Aging (Albany NY). 2022, 14(1): 286. 3. Xu L, Wang G, Shi R, et al.A cocktail of small molecules maintains the stemness and differentiation potential of conjunctival epithelial cells.The Ocular Surface.2023 4. He W, Zhu X, Xin A, et al. Long-term maintenance of human endometrial epithelial stem cells and their therapeutic effects on intrauterine adhesion. Cell & Bioscience. 2022, 12(1): 1-20. 5. Tao Z, Cui Y, Xu X, et al. FGFR redundancy limits the efficacy of FGFR4-selective inhibitors in hepatocellular carcinoma. Proceedings of the National Academy of Sciences. 2022, 119(40): e2208844119. 6. Schenke M, Prause H C, Bergforth W, et al. Human-Relevant Sensitivity of iPSC-Derived Human Motor Neurons to BoNT/A1 and B1. Toxins. 2021, 13(8): 585. 7. Housmans B A C, Neefjes M, Surtel D A M, et al. Synovial fluid from end-stage osteoarthritis induces proliferation and fibrosis of articular chondrocytes via MAPK and RhoGTPase signaling. Osteoarthritis and Cartilage. 2022
GPNA hydrochloride Vamotinib Nerol 2-Deoxy-D-glucose Anisomycin Aurintricarboxylic acid Terfenadine 3,4-Dicaffeoylquinic acid

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 TGF-β/Smad靶点化合物库 抗癌化合物库 细胞周期化合物库 细胞骨架化合物库 经典已知活性库 NO PAINS 化合物库 细胞重编程化合物库 口服活性化合物库 表型筛选靶点鉴定库

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Y-27632 146986-50-7 Apoptosis Cell Cycle/Checkpoint Cytoskeletal Signaling Stem Cells ROCK Rho-associated protein kinase ROK Inhibitor inhibit Rho-kinase Y 27632 Rho-associated kinase Y27632 inhibitor

 

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