Y-27632 2HCl 化学構造
分子量: 320.26

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製品表彰状(42)

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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]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity Description
Swiss 3T3 cells MWXGeY5kfGmxbjDBd5NigQ>? MUCxNEDPxE1? NX34TJRGOiCq NHPtcmpFVVOR M{\Y[GlvcGmkaYTzJJRp\SCjc4PlcYJtgSCxZjDtbYNzd3S3YoXs[ZMh[W6mIHnueIVzdWWmaXH0[UBncWyjbXXueJMhfG9iZn;ycUBmgHSnbnTl[EBxem:lZYPz[ZM>
N1E-115 M2Lub2Z2dmO2aX;uJGF{e2G7 MonPNVAh|ryP MUmyJIg> NEX6WnVFVVOR MUTJcohq[mm2czD0bIUh[XO|ZX3icJkhd2ZibXnjdo91fWK3bHXzJIFv\CCrboTldo1m\GmjdHWg[olt[W2nboTzJJRwKG[xcn2g[Zh1\W6mZXSgdJJw[2W|c3Xz
HeLa MmHDSpVv[3Srb36gRZN{[Xl? M321N|ExKM7:TR?= NVjH[oFJOzBibXnu MXLJcohq[mm2czD0bIUh\m:{bXH0bY9vKG:oIIP0doV{eyCoaXLldpMh[W6mIITo[UBie3OnbXLsfUBw\iC4aX7jeYxqdi2lb370ZYlvcW6pIH\vZ4FtKGGmaHXzbY9vew>?
CCL39 NWPjPVZnTnWwY4Tpc44hSXO|YYm= NHXTOW8{OCEQvF2= M2j4RlMxKG2rbh?= NWDNVGVMS2:vcHzleIVtgSCjYn;sbZNp\XNiYXP0bZZifGmxbjDv[kBP[S2KIHX4Z4hidmencjDOTGUyKGK7IHnueIVoemmwcx?=
Mesothelial cells from rat mesentery MXLJcpZie2m4ZTDBd5NigQ>? M2TkOFMxKM7:TR?= MVSyNEBp MVXCcI9kc3NiaX72ZZNqfmViYXP0bZZqfHl?
NIH3T3 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3mzNFExKM7:TR?= MnTpNVgh\A>? MlzoSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=>
Dbl-d NFTqe|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3sd202OTBizszN M3zjW|E5KGR? Ml\BV5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg>
Dbl-e MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3SydVExKM7:TR?= M4C5TVE5KGR? NVqx[oU4VW:mZYLheIVtgSCrbnjpZol1eyClZXzsJIdzd3e2aB?=
mNET1-d NEfJSWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\UZ4IyOCEQvF2= MUOxPEBl MX7TeJJwdmeueTDpcohq[mm2czDj[YxtKGe{b4f0bC=>
mNET1-e NFnHW3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2njXlExKM7:TR?= Mn7xNVgh\A>? NHPXTFhUfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>?
Ras-2 NHjC[oJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjTTIY5OTBizszN NHz6UHcyQCCm Mmf4V5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg>
Ras-4 NW\lNZJ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnDc5c2OTBizszN NGDKbFUyQCCm NX\RWXJzW3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh?
Src-1 M1;Te2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXexNEDPxE1? M2\0ZlE5KGR? NFGyNIlFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp
Src-4 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWKxNEDPxE1? M1;adFE5KGR? NGnOWZZFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp
NIH3T3 MlLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzjXpoyOCEQvF2= NUL1VIlTOThiZB?= NYTCOZpNTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>?
Src-1 NXvLNFc{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHxNVAh|ryP NEOwNWYyQCCm NWDs[ngxTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>?
Src-2 M4f6c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vsWlExKM7:TR?= NUSwUYhjOThiZB?= NGDXWVZFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp
SW620 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLPU2o2OTBizszN MnLqNVgh\A>? NWPhUmdITG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>?
HCT15 M2HwbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHBNFc3OTBizszN NX;PcY1OOThiZB?= NWjYV5ZYTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>?
HCT116 M1LScGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;KSFAyOCEQvF2= NV7jb2NCOThiZB?= Mn[3V5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg>
LS174T NUXUTZV{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILKPGMyOCEQvF2= M4n5T|E5KGR? M1vPZm1w\GW{YYTlcJkhcW6qaXLpeJMh[2WubDDndo94fGh?
Neonatal rat ventricular myocytes NFrKfoJHfW6ldHnvckBCe3OjeR?= M2LpSVExKM7:TR?= Mn34OFghcA>? MmHVTY5pcWKrdIOgSXQuOS2rbnT1Z4VlKGmwY4LlZZNmeyCrbjDwdo91\WmwIIP5cpRp\XOrczygZ4VtdCC|aYrlJIFv\CCveX;mbYJzcWyuYYKgc5Jo[W6renH0bY9v
Stellate Cell NFX6WYlHfW6ldHnvckBCe3OjeR?= MojoNlUh|ryP NH;oeXQyPSCvaX6= MWnJcohq[mm2czDmc5Ju[XSrb36gc4YhTi2jY4TpckB{fHKnc4Og[olj\XK|IHHu[EBxcG:|cHjvdplt[XSrb36gc4YhdXmxc3nuJIxq\2i2IHPoZYlv
Rat Vascular Smooth Muscle Cells M2LLfWZ2dmO2aX;uJGF{e2G7 NH7jZ2gyOCEQvF2= NX;IT2szOiCq M1G4UGlvcGmkaYTzJIFv\2mxdHXud4lvKEmLLXnu[JVk\WRiaInw[ZJ1em:yaIm=
PC3 MkDnSpVv[3Srb36gRZN{[Xl? M1;pSVI2KM7:TR?= NX7UPYg{OSCq Mlr2TY5lfWOnczDtc5JxcG:ub3fpZ4FtKGOqYX7n[ZM>
PC3 M2nJfG1q\3KjdHnvckBCe3OjeR?= M1O2elI2KM7:TR?= NFzGc2wyKGh? NFXDXWlKdmirYnn0d{B1cGViQl3GRk1EVSCjbnSgeIhmKEWJRj3zeIlufWyjdHXkJI1q\3KjdHnvci=>
PC3 NUjNc2ZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDyNlUh|ryP NH;Oc5YyPyCq M3HHSmRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg>
LNCaP MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2j6UVI2KM7:TR?= NYC3XJliOTdiaB?= M4LnemRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg>
Rat hepatic stellate cells Mn:1SpVv[3Srb36gRZN{[Xl? MkfBN|Ah|ryP NHjlOIk1QCCq MmPUSIlucW6rc3jld{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFXyb|ItKGGwZDDk[YNz\WG|ZYOgcoV4KESQQTDzfY51cGW|aYO=
Pancreatic acinar cells NX75TlluTnWwY4Tpc44hSXO|YYm= NHvJPHAyOMLizszN M2e3TFcxKG2rbh?= NGLrbWJRd3SnboTpZZRmeyCFQ1utd5RqdXWuYYTl[EBx[W6lcnXheIlkKGWweont[UB{\WO{ZYTpc44>
C2C12 MmL3SpVv[3Srb36gRZN{[Xl? NFn0OXQyOMLizszN MnP5OkBp M4HkNnBz\X[nboTzJJRp\SC|ZYLpcoUheGixc4Doc5J6dGG2aX;uJI9nKEmUUz2xJIlv\HWlZXSgZpkhcW6|dXzpckBidmRxb4KgWG5HNc7z
PC 12 NHvX[FFHfW6ldHnvckBCe3OjeR?= MlKyNVDDqM7:TR?= Ml73NlQhcA>? NH;SPGlCfHSnboXheIV{KGOjdHXjbI9t[W2rbnWgZolwe3mwdHjld4l{
Cynomolgus monkey embryonic stem cells Mmq3R5l1d3SxeHnjJGF{e2G7 M164fFIxKML3TR?= MX[yOEBp MkLhVJJwdW:2ZYOgZ5lGWyClZXzsJJN2en[rdnHs
TSGH 8301 Mlr2UYloemG2aX;uJGF{e2G7 NXPEe4dTOjBiwsXN MnfPNUBp NVXmO3V6UW6lcnXhd4V{KGOnbHygcYloemG2aX;u
Swiss3T3 MXXDc4xwdnlvZn;ycYlv\yCDc4PhfS=> MXexNEDDvU1? NYjjTnpJOTNiZB?= M{TMUmlv[3KnYYPld{Bxem:|dHH0[UBk\WyuIHPvcI9vgS2ob4LtbY5oKGGldHn2bZR6
HT22 NH7w[nNEgXSxdH;4bYMhSXO|YYm= MVexNEDDvU1? MmPqNVMhcA>? MYjQdo91\WO2czDh[4FqdnO2IHfseZRidWG2ZT3pcoR2[2WmIH7leZJwdmGuIHTlZZRp
Salivary gland stem cells MnzUSpVv[3Srb36gRZN{[Xl? MmPBNVAhyrWP NH\ERnM4KGR? MkfDVoVlfWOnczDTS3NEKHOnbnXzZ4Vv[2V?

... Click to View More Cell Line Experimental Data

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] Pretreatment with Y-27632 has a protective effect against tumor formation in albino mice with Ehrlich ascites carcinoma. [7]
臨床試験
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] [7]

動物モデル Male Wistar rats with spontaneous or induced hypertension; Swiss albino mice with Ehrlich ascites carcinoma
製剤 Dissolved in DMSO, and diluted in saline (Rat); 0.9% NaCl (Mice)
投薬量 30 mg/kg/day (Rat); 0-10 mg/kg (mice)
管理 Orally (Rat); i.p. (Mice)

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
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
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 64 mg/mL warmed (199.83 mM)
14 mg/mL (43.71 mM)
エタノール <1 mg/mL (<1 mM)
In vivo Saline 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 (1R,4r)-4-((R)-1-aminoethyl)-N-(pyridin-4-yl)cyclohexanecarboxamide dihydrochloride

カスタマーレビュー (4)


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Rating
Source J Clin Invest, 2014, 124(4), 1646-59. Y-27632 2HCl purchased from Selleck
Method Immunofluorescence
Cell Lines Nude mice
Concentrations 9 mg/kg
Incubation Time 4 weeks
Results The ROCK inhibitors fasudil and Y27632 prevented SCP2 cell bone metastasis in nude mice.

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Source Cell Rep, 2013, 3, 615-21. Y-27632 2HCl purchased from Selleck
Method NCC Explants
Cell Lines Neural crest cells
Concentrations
Incubation Time 16-20 h
Results In order to assess NCC migration, it measured the ROCK inhibitor Y27632, which could enhanced migration significantly. Remarkably, parallel loss of Xcnn2 through injection of Xcnn2MO reduced the Y27632-enhanced migration.

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Rating
Source J Mol Cell Cardiol, 2014, 67, 49-59. Y-27632 2HCl purchased from Selleck
Method SEM analyses, F-actin staining
Cell Lines Valve interstitial cells
Concentrations 8 uM
Incubation Time 24 h
Results In mineralizing media, cyclic strain induces a dramatic elongation of cells coupled to F-actin reorganization. It studied the effect of ROCK inhibitors (HA1100 and Y27632) on stretch-induced morphological changes. Treatment with HA1100 and Y27632 completely abolished cell area reduction as well as cell elongation in response to mechanical strain (B). Quantitative analyses of cell area revealed that mechanical strain significantly reduced cell area (A and B). Cells were enlarged and they round up into a more circular shape (C).

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Rating
Source Dev Biol, 2012, 370, 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 (42)

技術サポート&よくある質問(FAQ)

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description
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