Y-27632 2HCl 化学構造
分子量: 320.26

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製品説明

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  • 研究分野
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    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 Description
Swiss 3T3 cells MYnGeY5kfGmxbjDBd5NigQ>? MlnaNVAh|ryP M{jtWFIhcA>? NHj0fWVFVVOR MWHJcohq[mm2czD0bIUh[XO|ZX3icJkhd2ZibXnjdo91fWK3bHXzJIFv\CCrboTldo1m\GmjdHWg[olt[W2nboTzJJRwKG[xcn2g[Zh1\W6mZXSgdJJw[2W|c3Xz
N1E-115 NYj2OVIzTnWwY4Tpc44hSXO|YYm= M3fmdlExKM7:TR?= M1rYN|IhcA>? NF\UOIlFVVOR M3W3U2lvcGmkaYTzJJRp\SCjc4PlcYJtgSCxZjDtbYNzd3S3YoXs[ZMh[W6mIHnueIVzdWWmaXH0[UBncWyjbXXueJMhfG9iZn;ycUBmgHSnbnTl[EBxem:lZYPz[ZM>
HeLa MVvGeY5kfGmxbjDBd5NigQ>? Mm\hNVAh|ryP M1fQTFMxKG2rbh?= NIL3XpZKdmirYnn0d{B1cGViZn;ycYF1cW:wIH;mJJN1emW|czDmbYJmenNiYX7kJJRp\SCjc4PlcYJtgSCxZjD2bY5kfWyrbj3jc451[WmwaX7nJIZw[2GuIHHkbIV{cW:wcx?=
CCL39 MVTGeY5kfGmxbjDBd5NigQ>? NXvmXnJiOzBizszN M1TJVlMxKG2rbh?= NF7YbmhEd22ybHX0[Yx6KGGkb3zpd4hmeyCjY4TpeoF1cW:wIH;mJG5iNUhiZYjjbIFv\2W{IF7ISVEh[nliaX70[YdzcW6|
Mesothelial cells from rat mesentery MXHJcpZie2m4ZTDBd5NigQ>? MVuzNEDPxE1? NVS4PIdkOjBiaB?= NFXLR|dDdG:la4OgbY53[XOrdnWgZYN1cX[rdIm=
NIH3T3 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUGxNEDPxE1? NH;EVVgyQCCm NGDlOmlFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp
Dbl-d MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnUeZZbOTBizszN M3G4SFE5KGR? MnPmV5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg>
Dbl-e MlT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M375[lExKM7:TR?= MW[xPEBl MnrHUY9l\XKjdHXsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>?
mNET1-d M3:4WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnn5NVAh|ryP NU\Hc2V7OThiZB?= NVXiVlhzW3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh?
mNET1-e M{eyOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1G2fFExKM7:TR?= NXTWO2w6OThiZB?= NXnTWpk3W3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh?
Ras-2 NUn2NpZHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVixNEDPxE1? MmfiNVgh\A>? NULqRm8zW3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh?
Ras-4 M{SwSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml2yNVAh|ryP MnnXNVgh\A>? NHu1eHlUfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>?
Src-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHxNVAh|ryP MYGxPEBl M4G3W2Rw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg>
Src-4 NFjhXIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzuVGQyOCEQvF2= NYDaTogyOThiZB?= Mo\USI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=>
NIH3T3 NYjve29bT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILCRmEyOCEQvF2= NEPkSHYyQCCm M3LyOWRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg>
Src-1 M4DSRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\BNVAh|ryP MmDxNVgh\A>? NGLuSWpFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp
Src-2 NETaPZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TsSlExKM7:TR?= NILsdZQyQCCm M3LESGRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg>
SW620 NWnV[olPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYKxNEDPxE1? NFHT[YoyQCCm NUnsUHpETG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>?
HCT15 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml2wNVAh|ryP NX7XWoFZOThiZB?= NHWx[HRFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp
HCT116 M2X2c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITleG8yOCEQvF2= M2K1blE5KGR? NVW0dZh{W3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh?
LS174T NFfS[nhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LUNFExKM7:TR?= MX2xPEBl NUfB[mFqVW:mZYLheIVtgSCrbnjpZol1eyClZXzsJIdzd3e2aB?=
Neonatal rat ventricular myocytes NWXoTpgzTnWwY4Tpc44hSXO|YYm= M4HjelExKM7:TR?= M37LWVQ5KGh? MV7Jcohq[mm2czDFWE0yNWmwZIXj[YQhcW6lcnXhd4V{KGmwIIDyc5RmcW5ic4nueIhme2m|LDDj[YxtKHOrenWgZY5lKG27b3\pZpJqdGyjcjDvdodidmm8YYTpc44>
Stellate Cell M{jCSmZ2dmO2aX;uJGF{e2G7 NFX6fGMzPSEQvF2= MYKxOUBucW5? NFLxeHBKdmirYnn0d{Bnd3KvYYTpc44hd2ZiRj3hZ5RqdiC|dILld5Mh\mmkZYLzJIFv\CCyaH;zdIhwenmuYYTpc44hd2ZibYnvd4lvKGyrZ3j0JINp[Wmw
Rat Vascular Smooth Muscle Cells NX\kXpN2TnWwY4Tpc44hSXO|YYm= NHnOcYoyOCEQvF2= MnLmNkBp MmDjTY5pcWKrdIOgZY5ocW:2ZX7zbY4hUUlvaX7keYNm\CCqeYDldpRzd3CqeR?=
PC3 M3XEWGZ2dmO2aX;uJGF{e2G7 M4r6clI2KM7:TR?= NYjmRZZsOSCq MonnTY5lfWOnczDtc5JxcG:ub3fpZ4FtKGOqYX7n[ZM>
PC3 MmLjUYloemG2aX;uJGF{e2G7 MkPUNlUh|ryP NVvjelRZOSCq NXnRWVVLUW6qaXLpeJMhfGinIFLNSmIuS01iYX7kJJRp\SCHR1[td5RqdXWuYYTl[EBucWe{YYTpc44>
PC3 NX\iW|BtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;pNlUh|ryP NFL4T2YyPyCq M1;6dGRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg>
LNCaP MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnP3NlUh|ryP NHz3cXkyPyCq Mo[1SI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=>
Rat hepatic stellate cells NXnTeWI5TnWwY4Tpc44hSXO|YYm= M4i4clMxKM7:TR?= NUfuZYE3PDhiaB?= M2nZdGRqdWmwaYPo[ZMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDFdoszNCCjbnSg[IVkemWjc3XzJI5mfyCGTlGgd5lvfGinc3nz
Pancreatic acinar cells NVTCemdETnWwY4Tpc44hSXO|YYm= M2XlOVExyqEQvF2= MnnNO|AhdWmw NEflVndRd3SnboTpZZRmeyCFQ1utd5RqdXWuYYTl[EBx[W6lcnXheIlkKGWweont[UB{\WO{ZYTpc44>
C2C12 M2rjW2Z2dmO2aX;uJGF{e2G7 NIfWcnEyOMLizszN MYm2JIg> M{DmOnBz\X[nboTzJJRp\SC|ZYLpcoUheGixc4Doc5J6dGG2aX;uJI9nKEmUUz2xJIlv\HWlZXSgZpkhcW6|dXzpckBidmRxb4KgWG5HNc7z
PC 12 NWnEcpN2TnWwY4Tpc44hSXO|YYm= MV6xNOKh|ryP NV;DdWZWOjRiaB?= MlvRRZR1\W63YYTld{Bk[XSnY3jvcIFucW6nIHLpc5N6dnSqZYPpdy=>
Cynomolgus monkey embryonic stem cells M{\PXGN6fG:2b4jpZ{BCe3OjeR?= NFrtTpMzOCEEtV2= MWiyOEBp NGXxdYRRem:vb4Tld{BkgUWVIHPlcIwhe3W{dnn2ZYw>
TSGH 8301 NVTN[VRGVWmpcnH0bY9vKEG|c3H5 MknONlAhyrWP NVrNTnVVOSCq MlfkTY5kemWjc3XzJINmdGxibXnndoF1cW:w
Swiss3T3 NFfnXGpEd2yxbomt[o9zdWmwZzDBd5NigQ>? NYq2ZVB4OTBiwsXN MVixN{Bl MoCxTY5kemWjc3XzJJBzd3O2YYTlJINmdGxiY3;sc456NW[xcn3pcoch[WO2aY\peJk>
HT22 MkLyR5l1d3SxeHnjJGF{e2G7 NYPSbWR4OTBiwsXN NIfCcGoyOyCq Mn\nVJJwfGWldIOgZYdicW6|dDDncJV1[W2jdHWtbY5lfWOnZDDu[ZVzd26jbDDk[YF1cA>?
Salivary gland stem cells M37YeGZ2dmO2aX;uJGF{e2G7 NEXLfIcyOCEEtV2= Mo\uO{Bl MnvuVoVlfWOnczDTS3NEKHOnbnXzZ4Vv[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

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 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

カスタマーフィードバック (6)


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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 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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Source Cell Rep, 2015, 10(7), 1173-86. Y-27632 2HCl purchased from Selleck
Method FA images
Cell Lines C57BL/6J mice
Concentrations 10 mg/kg
Incubation Time 24 h
Results Immunohistochemistry showed staining for both ROCK1 and ROCK2 isoforms in infiltrated macrophages in the CNV lesions of mouse and monkey. The combination of growth-factor-induced corneal angiogenesis with in vivo acridine orange (AO) labeling of leukocytes allowed visualization of leukocyte extravasation from normal and angiogenic vessels in a chemotactic gradient. In MCP-1 implanted corneas, Y-27632 suppressed leukocyte transmigration, while selective ROCK2 inhibition did not. This is supported by our finding that Y-27632 affects cytoskeletal proteins, while selective ROCK2 inhibition.

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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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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.

文献中の引用 (42)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description
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