Y-27632 2HCl 化学構造
分子量: 320.26

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製品説明

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    ROCK製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法
  • Y-27632 2HClのメカニズム

製品の説明

生物活性

製品説明 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。
ターゲット 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 DescriptionPMID
Swiss 3T3 cells NVv3N4pNTnWwY4Tpc44hSXO|YYm= M{C5NFExKM7:TR?= MlLpNkBp NU\4dmtvTE2VTx?= MXfJcohq[mm2czD0bIUh[XO|ZX3icJkhd2ZibXnjdo91fWK3bHXzJIFv\CCrboTldo1m\GmjdHWg[olt[W2nboTzJJRwKG[xcn2g[Zh1\W6mZXSgdJJw[2W|c3Xz Ml3uPVY1PzZ3NB?=
N1E-115 MlXDSpVv[3Srb36gRZN{[Xl? M3zzSVExKM7:TR?= MoXXNkBp NVnpO2NETE2VTx?= MWjJcohq[mm2czD0bIUh[XO|ZX3icJkhd2ZibXnjdo91fWK3bHXzJIFv\CCrboTldo1m\GmjdHWg[olt[W2nboTzJJRwKG[xcn2g[Zh1\W6mZXSgdJJw[2W|c3Xz Mk\pPVY1PzZ3NB?=
HeLa NHXFWoxHfW6ldHnvckBCe3OjeR?= M4n5clExKM7:TR?= MUezNEBucW5? MYHJcohq[mm2czD0bIUh\m:{bXH0bY9vKG:oIIP0doV{eyCoaXLldpMh[W6mIITo[UBie3OnbXLsfUBw\iC4aX7jeYxqdi2lb370ZYlvcW6pIH\vZ4FtKGGmaHXzbY9vew>? M4m5c|k3PjhyN{K=
CCL39 MUTGeY5kfGmxbjDBd5NigQ>? MXyzNEDPxE1? NXmzWYx6OzBibXnu MY\Dc41xdGW2ZXz5JIFjd2yrc3jld{Bi[3SrdnH0bY9vKG:oIF7hMWgh\XilaHHu[4VzKE6KRUGgZpkhcW62ZXfybY5{ MlXWPVY6OzN6Mh?=
Mesothelial cells from rat mesentery MY\JcpZie2m4ZTDBd5NigQ>? NFLVU4M{OCEQvF2= MVSyNEBp M2PqRmJtd2OtczDpcpZie2m4ZTDhZ5Rqfmm2eR?= M2XWUlk6OzB6N{K=
NIH3T3 M4[zWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXnPZEyOCEQvF2= MnjyNVgh\A>? MYrEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To NWroT45nOTByMkGzPFY>
Dbl-d M2G3TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7kWmc3OTBizszN MW[xPEBl M1T2NHN1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp NFnycpAyODB{MUO4Oi=>
Dbl-e MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M374ZlExKM7:TR?= NHXSenEyQCCm NXSyWnVyVW:mZYLheIVtgSCrbnjpZol1eyClZXzsJIdzd3e2aB?= M4LFO|ExODJzM{i2
mNET1-d NVf6SpRvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnicmpOOTBizszN MW[xPEBl NXHaTmZVW3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh? NYL4XGxXOTByMkGzPFY>
mNET1-e NHTCOlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnseWVJOTBizszN NX\TNYY1OThiZB?= MlrOV5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NGjlTmUyODB{MUO4Oi=>
Ras-2 M17rUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7zclgyOCEQvF2= NVTYcnpoOThiZB?= NWL2R3dFW3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh? NH32epoyODB{MUO4Oi=>
Ras-4 M4mx[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUKxNEDPxE1? MoPhNVgh\A>? NEHlO3dUfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NUTT[2s6OTByMkGzPFY>
Src-1 M{jPcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDENVAh|ryP NFvlXpAyQCCm MXXEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To NHK3dIsyODB{MUO4Oi=>
Src-4 NXS1VndmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVqxNEDPxE1? NV\D[VI6OThiZB?= NXTQdpR4TG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? NIrIe28yODB{MUO4Oi=>
NIH3T3 NEfPTJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVuxNEDPxE1? MX:xPEBl NX3uNow2TG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? MnvlNVAxOjF|OE[=
Src-1 NX;Yb28zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTaNVAh|ryP M13wOlE5KGR? Mo\nSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> NHywWHMyODB{MUO4Oi=>
Src-2 M{LoUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELrXmcyOCEQvF2= NULwNY5SOThiZB?= NWDmOZg2TG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? NGrubJYyODB{MUO4Oi=>
SW620 Mn;uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjONVAh|ryP NFfHdpoyQCCm MYnEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To Mn7JNVAxOjF|OE[=
HCT15 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUixNEDPxE1? NWLTSml6OThiZB?= MljTSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> MlPyNVAxOjF|OE[=
HCT116 MonNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWSxNEDPxE1? NGDFUIUyQCCm NWnob5dTW3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh? MWGxNFAzOTN6Nh?=
LS174T NGfyWFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV2xNEDPxE1? MVSxPEBl MnPEUY9l\XKjdHXsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MmP0NVAxOjF|OE[=
Neonatal rat ventricular myocytes MYrGeY5kfGmxbjDBd5NigQ>? NHTFfWYyOCEQvF2= MUm0PEBp MoTQTY5pcWKrdIOgSXQuOS2rbnT1Z4VlKGmwY4LlZZNmeyCrbjDwdo91\WmwIIP5cpRp\XOrczygZ4VtdCC|aYrlJIFv\CCveX;mbYJzcWyuYYKgc5Jo[W6renH0bY9v NELZXWwyODN6Nk[xNy=>
Stellate Cell Ml\5SpVv[3Srb36gRZN{[Xl? MVWyOUDPxE1? NUDYZoJCOTVibXnu M1KyW2lvcGmkaYTzJIZwem2jdHnvckBw\iCILXHjeIlvKHO2cnXzd{BncWKncoOgZY5lKHCqb4PwbI9zgWyjdHnvckBw\iCveX;zbY4hdGmpaISgZ4hicW5? M1H6cFExPjByNEm2
Rat Vascular Smooth Muscle Cells MXTGeY5kfGmxbjDBd5NigQ>? MVexNEDPxE1? NIO1bIYzKGh? M3rpPWlvcGmkaYTzJIFv\2mxdHXud4lvKEmLLXnu[JVk\WRiaInw[ZJ1em:yaIm= NXLqbZdXOTB4NEKzNVc>
PC3 NGrnc|VHfW6ldHnvckBCe3OjeR?= MofWNlUh|ryP NXnhSnZYOSCq NVPJbotFUW6mdXPld{Bud3KyaH;sc4dq[2GuIHPoZY5o\XN? MnXvNVA4OjB2N{G=
PC3 MUjNbYdz[XSrb36gRZN{[Xl? MV[yOUDPxE1? MXKxJIg> NH7XSJVKdmirYnn0d{B1cGViQl3GRk1EVSCjbnSgeIhmKEWJRj3zeIlufWyjdHXkJI1q\3KjdHnvci=> NXrLcpROOTB5MkC0O|E>
PC3 NFzJ[3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYqyOUDPxE1? MmjrNVchcA>? NFvUWWRFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp NV30UIhrOTB5MkC0O|E>
LNCaP M{HXO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnoc2o1OjVizszN Mnz1NVchcA>? MWHEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To NH7Ye24yODd{MES3NS=>
Rat hepatic stellate cells NFL2UHFHfW6ldHnvckBCe3OjeR?= M3;C[lMxKM7:TR?= MUO0PEBp MlvnSIlucW6rc3jld{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFXyb|ItKGGwZDDk[YNz\WG|ZYOgcoV4KESQQTDzfY51cGW|aYO= MWWxNFg1PTZ4Mx?=
Pancreatic acinar cells MlLRSpVv[3Srb36gRZN{[Xl? M124d|ExyqEQvF2= M3v6NFcxKG2rbh?= Ml7UVI91\W62aXH0[ZMhS0ONLYP0bY12dGG2ZXSgdIFv[3KnYYTpZ{Bmdnq7bXWgd4VkemW2aX;u NI\1eGgyOjd2NUC4NC=>
C2C12 M130SGZ2dmO2aX;uJGF{e2G7 MmS2NVDDqM7:TR?= MUi2JIg> MXjQdoV3\W62czD0bIUhe2W{aX7lJJBpd3OyaH;yfYxifGmxbjDv[kBKWlNvMTDpcoR2[2WmIHL5JIlve3WuaX6gZY5lN2:{IGTOSk3PuQ>? NWf1W|hkOTZ{NkexNlQ>
PC 12 M4DYTGZ2dmO2aX;uJGF{e2G7 MlW3NVDDqM7:TR?= MXWyOEBp MnrGRZR1\W63YYTld{Bk[XSnY3jvcIFucW6nIHLpc5N6dnSqZYPpdy=> M4nRS|E3OjF7NEK0
Cynomolgus monkey embryonic stem cells NHrDfnhEgXSxdH;4bYMhSXO|YYm= MW[yNEDDvU1? NV3qdpRmOjRiaB?= NXvhUIlUWHKxbX;0[ZMh[3mHUzDj[YxtKHO3co\peoFt NWrmeXZFOTh7NEC4OVU>
TSGH 8301 NXfI[YpPVWmpcnH0bY9vKEG|c3H5 NUP0WIxKOjBiwsXN MX2xJIg> NHH6e5hKdmO{ZXHz[ZMh[2WubDDtbYdz[XSrb36= NFTTU3AyQTh7NkS3OS=>
Swiss3T3 NUnrVHZDS2:ub375MYZwem2rbnegRZN{[Xl? MnLsNVAhyrWP M4nxfFE{KGR? NUfLZ|M{UW6lcnXhd4V{KHC{b4P0ZZRmKGOnbHygZ49td267LX\vdo1qdmdiYXP0bZZqfHl? M17NbFIyPDZ2OUCy
HT22 NX:wblhwS3m2b4TvfIlkKEG|c3H5 M2fpN|ExKML3TR?= NIXnb|kyOyCq NUiycYFOWHKxdHXjeJMh[WejaX7zeEBodHW2YX3heIUucW6mdXPl[EBv\XW{b37hcEBl\WG2aB?= MX6yNlgyODh|NR?=
Salivary gland stem cells M4HxVWZ2dmO2aX;uJGF{e2G7 Mk\BNVAhyrWP Mn6xO{Bl M{D6XXJm\HWlZYOgV2dUSyC|ZX7ld4NmdmOn M{HBO|I2QDB2NU[w

... 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

プロトコル (参考用のみ)

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)
投与方法 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 warming (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

カスタマーフィードバック (4)


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Source , , J Clin Invest, 2014, 124(4): 1646-59. Y-27632 2HCl purchased from Selleck
Method Immunofluorescence
Cell Lines Nude mice
Concentrations 8 mg/kg
Incubation Time 4 weeks
Results By the fourth week, the bone metastasis burden of drug-treated mice was reduced 100-fold compared with control mice.

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Source Mol Neurobiol, 2015, 10.1007/s12035-014-9084-z. Y-27632 2HCl purchased from Selleck
Method Transwell cell invasion assay
Cell Lines Calu-6 cells
Concentrations 5, 10 uM
Incubation Time 24 h
Results Similar to SP600125, the Rho-associated, coiledcoil containing protein kinase (ROCK) inhibitor Y27632 can also directly alter cellular morphology and inhibit cell invasion and has synergistic effects when combined with vandetanib.

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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.

文献中の引用 (46)

Frequently Asked Questions

  • Question 1
    Is there any data about the Amax (maximum attraction luminosity) and extinction coefficient of this compound?

    Answer: The wavelength we used to test HPLC is 260nm while the extinction coefficient is unknown.

  • Question 2
    Could this product be used in cell culture? Do you have any reference for this application?

    Answer: Yes. The Y-27632 can be used in cell culture certainly. Here is the reference website: http://molpharm.aspetjournals.org/content/57/5/976.full.

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* 必須

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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