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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。
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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 247 | 现货 | |
2 mg | ¥ 352 | 现货 | |
5 mg | ¥ 578 | 现货 | |
10 mg | ¥ 745 | 现货 | |
25 mg | ¥ 1,450 | 现货 | |
50 mg | ¥ 2,650 | 现货 | |
100 mg | ¥ 3,290 | 现货 | |
200 mg | ¥ 4,810 | 现货 | |
500 mg | ¥ 7,580 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 555 | 现货 |
产品描述 | ZY-27632 is an orally potent, ATP-competitive inhibitor of ROCK-I and ROCK-II. Y-27632 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]. |
分子量 | 247.34 |
分子式 | C14H21N3O |
CAS No. | 146986-50-7 |
Smiles | C[C@@H](N)[C@H]1CC[C@@H](CC1)C(=O)Nc1ccncc1 |
密度 | 1.136 g/cm3 |
存储 | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | H2O: insoluble 10% DMSO+90% Saline: 2.47 mg/mL (9.99 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. DMSO: 45 mg/mL (181.94 mM) | ||||||||||||||||||||||||||||||||||||||||
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