Y-27632 2HCl

Y-27632 2HClはRho関連プロテインキナーゼ1(ROCK1、p160ROCK)選択阻害剤、Kiが140nMになる。

目録号S1049
5 5 1レビュー 10製品表彰状
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Y-27632 2HCl 化学構造
分子量: 320.26

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製品情報

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製品の説明

生物活性

情報 Y-27632 2HClはRho関連プロテインキナーゼ1(ROCK1、p160ROCK)選択阻害剤、Kiが140nMになる。
目標 ROCK1 ROCK2
IC50 140 nM (Ki) [1] 300 nM (Ki) [6]
In vitro試験 Y-27632 2HCl inhibits ROCK-II while displaying little activity against PKC, cAMP-dependent protein kinase and myosin light-chain kinase (MLCK) with Ki of 26 μM, 25 μM and > 250 μM, respectively, as well as PKA activated by another Rho-family GTPase member, Cdc42. Y-27632 2HCl inhibits smooth-muscle contraction induces by various agonists including phenylephrine, histamine, acetylcholine, serotonin, endothelin, and thromboxane with IC50 of 0.3-1 μM, by selectively inhibiting Ca2+ sensitization. Y-27632 2HCl suppresses Rho-induced, p160ROCK-mediated formation of stress fibres in cultured cells. [1] Y-27632 2HCl treatment blocks both Rho-mediated activation of actomyosin and LPA-stimulated invasive activity of MM1 cells in a concentration-dependent manner. [2] Y-27632 2HCl treatment is not only sufficient to initiate formation of exuberant axonal processes but also facilitates axonal maturation during the very early stages of axonogenesis, while largely sparing axon elongation. [3] In human embryonic stem (hES) cells, Y-27632 2HCl treatment at 10 μM markedly diminishes dissociation-induced apoptosis even in serum-free suspension (SFEB) culture, increases cloning efficiency (from ~1% to ~27%), facilitates subcloning after gene transfer, and enables SFEB-cultured hES cells to survive and differentiate into Bf1+ cortical and basal telencephalic progenitors. [4]
In vivo試験 Oral administration of Y-27632 2HCl at 30 mg/kg significantly decreases the blood pressure in a dose-dependent manner in spontaneous hypertensive rats, renal hypertensive rats, as well as deoxycorticosterone acetate (DOCA)-salt hypertensive rats. [1] When Y-27632 2HCl is continuously administered at a rate of 0.55 μL per hour by implanted pumps for 11 days tumor cell invasion (MM1 cells expressing Val14-RhoA in rats) is significantly delayed. [2] By inhibiting ROCK, Y-27632 2HCl treatment attenuates hypoxia-induced angiogenesis and vascular remodeling in the pulmonary circulation. [5]
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特集

推薦された実験操作 (公開の文献だけ)

キナーゼアッセイ: [1]

Phosphorylation reactions The p160ROCK is expressed in COS cells as tagged full-length proteins, and immunoprecipitated by the use of anti-tag antibodies. The p160ROCK (30 ng) is incubated with 40 μM [γ-32P]ATP (3.3 Ci/mmol) and with 3 μg of either histone (HF2A), dephosphorylated casein or MBP in the presence of various concentrations of Y-27632 2HCl at 30 °C in a total volume of 31 μL. A 7 μL aliquot is taken at 0, 5, 10, and 20 minutes, mixed with an equal volume of 2 × Laemmli sample buffer, and applied to SDS-PAGE. The gel is stained with Commassie Blue, dried and subjected to analysis by a Bioimage Analyzer BAS2000. The Y-27632 2HCl concentration required to inhibit p160ROCK activity by 50% (IC50 value) is obtained. Ki value is calculated according to the equation, Ki = IC50/(1 + S/Km), where S and Km represent concentrations of and Km value for ATP.

動物実験: [1]

動物モデル Male Wistar rats with spontaneous or induced hypertension
製剤 Dissolved in DMSO, and diluted in saline
投薬量 30 mg/kg/day
管理 Orally
1

参考

化学情報

Download Y-27632 2HCl SDF
分子量 320.26
化学式

C14H21N3O.2HCl

CAS No. 129830-38-2
別名 N/A
溶解度 (25°C)
  • DMSO 64 mg/mL
  • 水 64 mg/mL
  • エタノール <1 mg/mL
保管 2年 -20°C
6月-80°Cin DMSO
化学名 (1R,4r)-4-((R)-1-aminoethyl)-N-(pyridin-4-yl)cyclohexanecarboxamide dihydrochloride

研究分野

カスタマーレビュー (1)


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Source Dev Biol, 2012, 370(1), 33-41. Y-27632 2HCl purchased from Selleck
Method Embryo studies
Cell Lines chicken neural tube
Concentrations 5 mM
Incubation Time
Results Rho kinase inhibitor Y-27632 prevents apical rounding during mitosis.

製品表彰状 (10)

  • Generation of haploid embryonic stem cells from Macaca fascicularis monkey parthenotes. [Yang H, et al. Cell Res 2013;23(10):1187-200]

    PubMed: 23856644
  • A fully defined and scalable 3D culture system for human pluripotent stem cell expansion and differentiation. [Lei Y, et al. Proc Natl Acad Sci USA 2013;110(52):E5039-48]

    PubMed: 24248365
  • Leveraging Nanochannels for Universal, Zero-Order Drug Delivery In Vivo. [Ferrati S, et al. J Control Release 2013;172(3):1011-9]

    PubMed: 24095805
  • Mechanical strain induces the production of spheroid mineralized microparticles in the aortic valve through a RhoA/ROCK-dependent mechanism. [Bouchareb R ,et al. J Mol Cell Cardiol 2013;67C:49-59]

    PubMed: 24368096
  • Generation of organized anterior foregut epithelia from pluripotent stem cells using small molecules. [Nicola A, et al. Stem Cell Research 2013;11(3):1003-12]

    PubMed: 23917481
  • Apical movement during interkinetic nuclear migration is a two-step process. [Spear PC, et al. Dev Biol 2012;370(1):33-41]

    PubMed: 22884563
  • Cas9 effector-mediated regulation of transcription and differentiation in human pluripotent stem cells. [Kearns NA ,et al. Development 2013;10.1242/dev.103341]

    PubMed: 24346702
  • CELLULAR PATHWAYS INVOLVED IN EPITHELIAL-TO-MESENCHYMAL TRANSITIONS IN NEURAL CREST CELLS [Li, Shen University of Maryland ;University of Maryland]

  • Select G-protein-coupled receptors modulate agonist-induced signaling via a ROCK, LIMK, and β-arrestin 1 pathway. [Mittal N, et al. Cell Rep 2013;5(4):1010-21]

    PubMed: 24239352
  • Calponin 2 acts as an effector of noncanonical Wnt-mediated cell polarization during neural crest cell migration. [Ulmer B, et al. Cell Rep 2013;3(3):615-21]

    PubMed: 23499442

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顧客がするかもしれない質問に対する答えは、指示を取り扱っている阻害剤で見つかります。話題は、貯蔵液(阻害剤と特別な注意を細胞ベースの分析法と動物のために必要とする問題を保存することは実験します)を準備する方法を含みます。

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