Y-27632
作者：齊岳
發(fā)布時間：2023-09-05
08:51:47
點擊數(shù)：
產(chǎn)品名稱：Y-27632
產(chǎn)品描述：
| 產(chǎn)品描述 | Y-27632 is a selective ATP-competitive inhibitor of ROCK-I and ROCK-II. |
| 靶點活性 | ROCK-II:300 nM(ki), ROCK-I:220 nM(ki) |
| 體外活性 | Y-27632 inhibits the ROCK family of kinases 100 times more potently than other kinases including protein kinase C, cAMP-dependent kinase and myosin light chain kinase. Y-27632 prolongs the lag time and delays the appearance of BrdU-labeled cells in a concentration-dependent manner, delays of about 1 and 4 h are noticed in the Swiss 3T3 cells treated with 10 and 100 μM Y-27632, respectively[1]. Y-27632 promotes neuronal differentiation of adipose tissue-derived stem cells (ADSCs). The percentages of neuroal-like cells achieved a peak in the 5.0 μM Y-27632 induced group when compared to 1.0 and 2.5 μM Y-27632 induced groups[2]. |
| 體內(nèi)活性 | Y-27632 (5 and 10?mg/kg) significantly prolongs the onset time of myoclonic jerks when compare with saline group. Y-27632 (5 and 10?mg/kg) significantly prolongs the onset time of clonic convulsions when compare with saline group[3]. Treatment with Dimethylnitrosamine (DMN) results in a significant decrease in rat body and liver weight (DMN-S group) compared with control animals (S-S group). Oral Y27632 (30 mg/kg) essentially prevents this DMN-induced rat body and liver weight loss (DMN-Y group)[4]. |
| 激酶實驗 | 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]. |
| 細胞實驗 | 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]. |
| 化合物與蛋白結(jié)合的復(fù)合物 |
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 |
存儲
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 100 mM
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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