Y-27632 2HCl 化学構造
分子量: 320.26

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製品説明

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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 DescriptionPMID
Swiss 3T3 cells MWjGeY5kfGmxbjDBd5NigQ>? NUXzRVhEOTBizszN MW[yJIg> M{fwb2ROW09? MXrJcohq[mm2czD0bIUh[XO|ZX3icJkhd2ZibXnjdo91fWK3bHXzJIFv\CCrboTldo1m\GmjdHWg[olt[W2nboTzJJRwKG[xcn2g[Zh1\W6mZXSgdJJw[2W|c3Xz MlvxPVY1PzZ3NB?=
N1E-115 MXPGeY5kfGmxbjDBd5NigQ>? NF31W4YyOCEQvF2= NWLJeXZ[OiCq MWHEUXNQ NV60NW1LUW6qaXLpeJMhfGinIHHzd4Vu[my7IH;mJI1q[3KxdIXieYxmeyCjbnSgbY51\XKvZXTpZZRmKG[rbHHt[Y51eyC2bzDmc5JuKGW6dHXu[IVlKHC{b3Pld5Nmew>? MUW5OlQ4PjV2
HeLa MYDGeY5kfGmxbjDBd5NigQ>? M1f1XlExKM7:TR?= M4XZOlMxKG2rbh?= NXvkUnpMUW6qaXLpeJMhfGinIH\vdo1ifGmxbjDv[kB{fHKnc4Og[olj\XK|IHHu[EB1cGViYYPz[Y1jdHlib3[geolv[3WuaX6tZ49vfGGrbnnu[{Bnd2OjbDDh[Ihme2mxboO= MYG5OlY5ODd{
CCL39 Mni4SpVv[3Srb36gRZN{[Xl? M3K4NFMxKM7:TR?= M2DmSlMxKG2rbh?= NIridYtEd22ybHX0[Yx6KGGkb3zpd4hmeyCjY4TpeoF1cW:wIH;mJG5iNUhiZYjjbIFv\2W{IF7ISVEh[nliaX70[YdzcW6| Mmf6PVY6OzN6Mh?=
Mesothelial cells from rat mesentery M3X1b2lvfmG|aY\lJGF{e2G7 MoPWN|Ah|ryP MYWyNEBp M13X[GJtd2OtczDpcpZie2m4ZTDhZ5Rqfmm2eR?= NVriUGpFQTl|MEi3Ni=>
NIH3T3 NF74[npIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXoXWYyOCEQvF2= NH\KUYkyQCCm NFTPdnFFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp M{jNXVExODJzM{i2
Dbl-d Mm\NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17relExKM7:TR?= MmPqNVgh\A>? NXexVIFiW3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh? M1\uVVExODJzM{i2
Dbl-e M3fXSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYWxNEDPxE1? M3;RSFE5KGR? MmnWUY9l\XKjdHXsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NYm3c5d7OTByMkGzPFY>
mNET1-d NGL5PGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYSxNEDPxE1? MWCxPEBl NEHLNZlUfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MXexNFAzOTN6Nh?=
mNET1-e NUX4RnpFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlj4NVAh|ryP M1PEblE5KGR? NU\GOZZNW3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh? M1S3NlExODJzM{i2
Ras-2 Mo\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYexNEDPxE1? MnjCNVgh\A>? MnzaV5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NGPiPFgyODB{MUO4Oi=>
Ras-4 NIHXOYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2frUFExKM7:TR?= NYnoVVVUOThiZB?= MV\TeJJwdmeueTDpcohq[mm2czDj[YxtKGe{b4f0bC=> NGHHPZcyODB{MUO4Oi=>
Src-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LBPVExKM7:TR?= MWqxPEBl MWjEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To NH;ONZEyODB{MUO4Oi=>
Src-4 NVG4OZJJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zFeVExKM7:TR?= MmnpNVgh\A>? MX\Ec4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To NVnQVGRmOTByMkGzPFY>
NIH3T3 NFjndnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvGcmgyOCEQvF2= M{LSPVE5KGR? MVXEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To MVGxNFAzOTN6Nh?=
Src-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{ezU|ExKM7:TR?= NVf4R41DOThiZB?= M2C3NWRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> NYTyZ|N{OTByMkGzPFY>
Src-2 MmfBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUmxNEDPxE1? M4nNeFE5KGR? NYDZTpJrTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? MkDDNVAxOjF|OE[=
SW620 M3HNW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVOxNEDPxE1? M1nodVE5KGR? MYLEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To NYn4XVdsOTByMkGzPFY>
HCT15 Mn\PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\UXVExKM7:TR?= NXLxN5RIOThiZB?= NGfoS2tFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp NYPDe4VOOTByMkGzPFY>
HCT116 Mn7VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHzU3dQOTBizszN NYDoOWdHOThiZB?= M1n6R3N1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp NHm0UYcyODB{MUO4Oi=>
LS174T M3u2cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\PZWUyOCEQvF2= NY\jRZYyOThiZB?= MWnNc4RmemG2ZXz5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp MV[xNFAzOTN6Nh?=
Neonatal rat ventricular myocytes NF;t[|ZHfW6ldHnvckBCe3OjeR?= NHrkUVEyOCEQvF2= NILLSIE1QCCq NEOwNJdKdmirYnn0d{BGXC1zLXnu[JVk\WRiaX7jdoVie2W|IHnuJJBzd3SnaX6gd5lvfGinc3nzMEBk\WyuIIPpfoUh[W6mIH35c4Zq[nKrbHzhdkBwemejbnn6ZZRqd25? MVuxNFM5PjZzMx?=
Stellate Cell NF3Hd3hHfW6ldHnvckBCe3OjeR?= MmrENlUh|ryP MVexOUBucW5? MWjJcohq[mm2czDmc5Ju[XSrb36gc4YhTi2jY4TpckB{fHKnc4Og[olj\XK|IHHu[EBxcG:|cHjvdplt[XSrb36gc4YhdXmxc3nuJIxq\2i2IHPoZYlv MlPKNVA3ODB2OU[=
Rat Vascular Smooth Muscle Cells MYnGeY5kfGmxbjDBd5NigQ>? NHHSU|IyOCEQvF2= M4nzNVIhcA>? NXXBclZTUW6qaXLpeJMh[W6paX;0[Y5{cW5iSVmtbY5lfWOnZDDofZBmenS{b4DofS=> NXTIdZdxOTB4NEKzNVc>
PC3 NYTzSJhoTnWwY4Tpc44hSXO|YYm= Mnf5NlUh|ryP NUjGUXYxOSCq MXjJcoR2[2W|IH3vdpBpd2yxZ3njZYwh[2ijbnfldy=> NHrTeVcyODd{MES3NS=>
PC3 MVLNbYdz[XSrb36gRZN{[Xl? NY\ZdHluOjVizszN M1XQPFEhcA>? NWTEV5pYUW6qaXLpeJMhfGinIFLNSmIuS01iYX7kJJRp\SCHR1[td5RqdXWuYYTl[EBucWe{YYTpc44> MlzlNVA4OjB2N{G=
PC3 M1;xRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTBUJozPSEQvF2= M1LPSlE4KGh? NWHLXnpoTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? NG[xUWcyODd{MES3NS=>
LNCaP NIDxXYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVSwTG1QOjVizszN M3zjV|E4KGh? Mn3lSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> MWGxNFczODR5MR?=
Rat hepatic stellate cells M2\ic2Z2dmO2aX;uJGF{e2G7 M3zFelMxKM7:TR?= MVq0PEBp M3faV2RqdWmwaYPo[ZMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDFdoszNCCjbnSg[IVkemWjc3XzJI5mfyCGTlGgd5lvfGinc3nz NUH3TXhXOTB6NEW2OlM>
Pancreatic acinar cells NVXIdoVWTnWwY4Tpc44hSXO|YYm= NXzlSo1wOTEEoN88US=> NEnnPWQ4OCCvaX6= M1\1WnBwfGWwdHnheIV{KEOFSz3zeIlufWyjdHXkJJBidmO{ZXH0bYMh\W68eX3lJJNm[3KndHnvci=> Ml3DNVI4PDVyOEC=
C2C12 NUPkXGIyTnWwY4Tpc44hSXO|YYm= Mn3SNVDDqM7:TR?= MknaOkBp M2C3e3Bz\X[nboTzJJRp\SC|ZYLpcoUheGixc4Doc5J6dGG2aX;uJI9nKEmUUz2xJIlv\HWlZXSgZpkhcW6|dXzpckBidmRxb4KgWG5HNc7z MYGxOlI3PzF{NB?=
PC 12 NVHVcWVGTnWwY4Tpc44hSXO|YYm= Mn3BNVDDqM7:TR?= MUmyOEBp MYTBeJRmdnWjdHXzJINifGWlaH;sZY1qdmViYnnvd5lvfGinc3nz NYLGdIRQOTZ{MUm0NlQ>
Cynomolgus monkey embryonic stem cells NXvQXpdpS3m2b4TvfIlkKEG|c3H5 Mn23NlAhyrWP NYftZVF2OjRiaB?= MoTBVJJwdW:2ZYOgZ5lGWyClZXzsJJN2en[rdnHs Mmn1NVg6PDB6NUW=
TSGH 8301 MWrNbYdz[XSrb36gRZN{[Xl? NUDDc214OjBiwsXN Mn\DNUBp M1;qbmlv[3KnYYPld{Bk\WyuIH3p[5JifGmxbh?= NUnKS3prOTl6OU[0O|U>
Swiss3T3 NGjUWZZEd2yxbomt[o9zdWmwZzDBd5NigQ>? MoTJNVAhyrWP MYKxN{Bl M1XKW2lv[3KnYYPld{Bxem:|dHH0[UBk\WyuIHPvcI9vgS2ob4LtbY5oKGGldHn2bZR6 NXrsdIw3OjF2NkS5NFI>
HT22 NFrBSIREgXSxdH;4bYMhSXO|YYm= M3u1PVExKML3TR?= MoPCNVMhcA>? M3nGU3Bzd3SnY4TzJIFo[Wmwc4Sg[4x2fGGvYYTlMYlv\HWlZXSgcoV2em:wYXyg[IVifGh? MWWyNlgyODh|NR?=
Salivary gland stem cells NVz3WolwTnWwY4Tpc44hSXO|YYm= NIr0VYMyOCEEtV2= MUS3JIQ> M{LYUXJm\HWlZYOgV2dUSyC|ZX7ld4NmdmOn Mn[3NlU5ODR3NkC=

... 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 (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 (45)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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