Research Area
Product Type
United States ( Change Country )
Y-27632 2HCl Chemical Structure
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Biological Activity
| Information | Y-27632 2HCl is ROCK inhibitor, as a novel bronchodilator. Y27632 is available with IC50 of 3.3±0.25 μM and 2.8±0.2 μM in human and rabbit tissues, respectively. | |||||
|---|---|---|---|---|---|---|
| Targets | p160ROCK | ROCK-II | ||||
| IC50 | 0.14 μM | 0.8 μM [1] | ||||
| In vitro | Y-27632 inhibits Walker 256 cell chemotaxis towards the serum-free conditioned medium in a dose-dependent fashion (5-40 μM). Y-27632 also inhibits the chemoinvasion activity of Walker 256 cells as measured using Matrigel chamber in a dose-dependent fashion (5-40 μM). The lowest concentration of Y-27632 used, 5 μM, significantly inhibits both chemotaxis and chemoinvasion. Treatment with 10 μM of Y-27632 evokes drastic morphologic changes in Walker 256 cells. Y-27632 treatment slightly inhibits Walker 256 cell colony formation in soft agar. The number of large-sized (diameter > 300 μm) colonies is reduced by Y-27632 treatment doses higher than 5 μM. Y-27632 inhibits the myosin light chain phosphorylation level in a dose-dependent fashion. [1] Y-27632 concentrations less than 20μM result in minimal neurotoxicity.[2] Y-27632 treatment also reduces expression of SMA mRNA in cultured renal fibroblasts in a dose-dependent manner, but reductions of I collagen and TGF- mRNA levels in cultured renal fibroblasts are not significant. Y-27632 does not show an inhibitory effect on proliferation of mouse renal fibroblasts even at a dose of 200 μM, and shows cytotoxicity at a dose of 2 mM. Y-27632 abrogates MCP-1–induced macrophage migration in a dose-dependent manner. Ang II stimulates macrophage migration and it is significantly suppressed by Y-27632. Y-27632 causes significant concentration-dependent inhibition of HTF-mediated collagen gel contraction in the presence of serum. [3] | |||||
| In vivo | Continuous intrathecal infusion of Y-27632 by the Alzet mini-pump causes the deaths of three of six rats, each of which receives 100 mg of Y-27632 in total. The three dead rats suffer severe hydrocephalus. Continuous intrathecal administration of 50 mg/200 μL Y-27632 in the three surviving rats does not seem to have any adverse effects on brain tissue, as histologic examination of various brain regions (medulla, ventricle, front bases, and cistern) after continuous intrathecal administration of 50 mg/200 μL Y-27632 does not reveal any acute or chronic abnormalities. [1] Although the group which receives continuous intrathecal infusion of Y-27632 shows a longer mean survival period than the control group, the difference does not reach statistical significance. Continuous intrathecal infusion of FdUrd (200 μg/200 μL) significantly increases the survival time of treated rats compared with that of the control group, whereas animals which receive the treatment regimen combining continuous intrathecal infusion of FdUrd (200 μg/200 μL) with Y-27632 (50 mg/200 μL) show significantly longer survival times than do the group receiving continuous intrathecal FdUrd only. The rats which receive continuous intrathecal Y-27632 clearly show minimal invasion of disseminated tumor cells into parenchymal tissues within the basal region of the midbrain and pons. [2] | |||||
| Clinical Trials | ||||||
| Features | ||||||
Protocol
Kinase Assay: [1]
| Kinase Assay | 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 μg of histone type 2 as substrates in the absence or presence of various concentrations of Y-27632 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. PKCα 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 Y-27632 at 30 ℃ 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 4× Laemmli sample buffer. |
|---|
Cell Assay: [2]
| Cell lines: | Walker 256 cells |
|---|---|
| Concentrations: | First dissolved in PBS and then diluted to 5-40 μM in the culture media |
| Incubation Time: | 7 days |
| Method: | Walker 256 cells (5 × 103 cells) are plated into 24-well plates and cultured in DMEM with 10% FCS for 24 hours. Then the cells are treated with Y-27632 for 7 days. The culture media is changed every 2 days. Cell numbers are measured every 24 hours by the WST-8 (2-(2-methoxy-4-nitrophenyl)-3-(4-nitrophenyl)-5-(2,4-disulfophenyl)-tetrazoliu, monosodium salt) assay. |
Animal Study:[2]
Chemical Information
| Molecular Weight (WM): | 320.26 |
|---|---|
| Formula: | C14H21N3O*2HCl |
| CAS No.: | 129830-38-2 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥50mg/mL |
| Water ≥50mg/mL | |
| Ethanol ≥12mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
Research Area
Notes:
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