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- CAS号：
129830-38-2
- 规格：
1mg/1mLx10mM(inDMSO)/2mg/5mg/10mg/25mg/50mg/100mg/200mg/500mg
| 规格： | 1mg | 产品价格： | ￥214.0 |
|---|---|---|---|
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥509.0 |
| 规格： | 2mg | 产品价格： | ￥297.0 |
| 规格： | 5mg | 产品价格： | ￥462.0 |
| 规格： | 10mg | 产品价格： | ￥596.0 |
| 规格： | 25mg | 产品价格： | ￥1160.0 |
| 规格： | 50mg | 产品价格： | ￥2120.0 |
| 规格： | 100mg | 产品价格： | ￥2632.0 |
| 规格： | 200mg | 产品价格： | ￥3832.0 |
| 规格： | 500mg | 产品价格： | ￥6056.0 |
Product Introduction
Bioactivity
| 名称 | Y-27632 dihydrochloride |
| 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. |
| 细胞实验 | HeLa cells are plated at a density of 3×10^4 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) or vehicle is added and the cells are incubated for another 30 min [1]. |
| 激酶实验 | Recombinant ROCK1/2, 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 phosphatidylserine, 50 ng/mL 12-O-tetradecanoyl phorbol-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]. |
| 动物实验 | A group of animals was injected with a single dose of pentylenetetrazole (PTZ, 65?mg/kg) to investigate if the two Rho-kinase inhibitors, fasudil, and Y-27632, changed the onset of PTZ seizures. Fasudil, Y-27632 or saline was given intraperitoneally 30?min before the PTZ injection. Each mouse was then observed for a 15-min period to measure the onset of the first myoclonic jerk, the onset of the first clonic convulsion and the occurrence of tonic hindlimb extension. Some of the animals died after tonic hindlimb extension, which is an expected outcome of acute PTZ injection. After the observation period, all animals were killed by halothane anesthesia [5]. Seven-week-old male Wistar rats were anesthetized with sodium pentobarbital. A silver clip (0.2 mm in diameter) was placed on the left renal artery in the preparation of the renal hypertensive rats. In the preparation of the DOCA-salt hypertensive rats, the left kidney was removed and a DOCA pellet (50 mg) was implanted subcutaneously. The DOCA rats were then fed an 8% salt diet. Rats from both groups were used after 8 weeks in the experiments, together with a male, 17–22-week old spontaneously hypertensive rats. The average systolic pressure in these groups of hypertensive rats ranged from 209 to 237 mm Hg, and no significant difference was found between groups. Eight-week-old male Wistar rats were used as controls. Their average systolic pressure was 139 mm Hg. Y-27632was administered orally. The systolic blood pressure was measured by the tail cuff method at 1, 3, 5, 7 and 24 h. The rats were prewarmed to 40 8C for 10 min before each measurement. No toxicity was found in rats treated with 30 mg kg?1 of Y-27632 administered per os once per day for 10 days [4]. |
| 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] |
| 存储条件 | Keep away from moisture,Keep away from direct sunlight,Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (15.61 mM), Sonication is recommended. DMSO : 255 mg/mL (796.23 mM), Sonication is recommended. H2O : 32.03 mg/mL (100.01 mM), Sonication is recommended. |
| 关键字 | Y-27632 Dihydrochloride | Y27632 Dihydrochloride | Y-27632 | Y27632 | Y 27632 Dihydrochloride | Y 27632 | transition-like | stem | ROK | ROCK2 | ROCK1 (p160ROCK) | ROCK | Rho-kinase | Rho-associated protein kinase | Rho-associated kinase | pluripotent | orally | modulation | mesendodermal | lineage | Inhibitor | inhibit | hIPSCs | epithelial-mesenchymal | cells | ATP-competitive | Apoptosis | active |
| 相关产品 | Formamide | Urea | Sodium Molybdate | Dimethyl phthalate | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Metronidazole | Sildenafil citrate | Citric Acid Triammonium | Stavudine | Tamoxifen |
| 相关库 | Inhibitor Library | Anti-Cancer Active Compound Library | Bioactive Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Neural Regeneration Compound Library | Highly Selective Inhibitor Library | Anti-Aging Compound Library | TGF-beta/Smad Compound Library | Membrane Protein-targeted Compound Library | Orally Active Compound Library | Wnt/Hedgehog/Notch Compound Library |
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相关实验
Nature Methods-让胚胎干细胞茁壮成长，一个神奇的小分子配方介绍
assay qHTS) ，通过CTG(CELL TITER-GLO)发光法评估15, 333种化合物对细胞活力的影响，发现总共有113种类型能够提高细胞存活率。而其中Chroman 1对ROCK通路比Y-27632具有更好的抑制效果和选择性。随后，作者从113个活性化合物中，挑选了29个作用不同靶点的化合物进行了组合小分子基质筛选(Combinatorial small-molecule matrix screening)，发现Chroman 1与Caspase阻滞剂Emricasan有显著的协同
Cell Rep Med：李振斐 / 吴登龙 / 唐惠儒团队发现黄体酮是前列腺癌的促癌代谢物，提出晚期治疗新策略
物；基于黄体酮的代谢和功能研究，研究人员发现小分子化合物 biochanin-A（BCA）能够靶向抑制代谢酶 3βHSD1，进而抑制黄体酮合成、克服药物耐受；并指出患者血液中黄体酮的丰度是阿比特龙疗效的潜在预测型生物标志物。 去势治疗联合药物阿比特龙能够将患者体内的雄激素控制在非常低的水平，这为寻找独立于雄激素的新促癌代谢物提供了可行性。研究人员利用接受阿比特龙和去势治疗的患者样本进行代谢组学研究。在 6625 个代谢物中，代谢物黄体酮在阿比特龙治疗后显著升高。 进一步的机制研究发现，高浓度的黄体
砷剂疗法的前世今生：「吃最毒的药，治最难的病」，「砒霜」抗癌再登 Cell 子刊
Allosteric Site 的研究 [8]，报道了 ATO 是如何通过砷原子填补明星抑癌基因 p53 的空腔，以维持后者的稳定，并恢复 p53 抑癌功能的全新机制。这意味着砷剂在治疗结构突变型 p53 癌症中具有巨大的潜力。（推荐阅读：瑞金医院卢敏团队实质性获得「靶向治疗领域的圣杯」——p53 靶向化合物）全世界一半的癌症患者具有 p53 突变，其中带有结构性突变的人群也不在少数。利用精准医疗，现代医学能够快速的识别出适合使用砷剂治疗的人，并造福广大的癌症患者。该发现也使得砷剂的未来，比 APL 更加广阔
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化合物 Y-27632 dihydrochloride【129830-38-2】
￥214 - 6056
