Y-27632 2HCl 化学構造
分子量: 320.26

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製品説明

  • Compare ROCK Inhibitors
    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 MYHGeY5kfGmxbjDBd5NigQ>? NF3iVmsyOCEQvF2= NEThUWozKGh? NGTsW5VFVVOR MX3Jcohq[mm2czD0bIUh[XO|ZX3icJkhd2ZibXnjdo91fWK3bHXzJIFv\CCrboTldo1m\GmjdHWg[olt[W2nboTzJJRwKG[xcn2g[Zh1\W6mZXSgdJJw[2W|c3Xz NXq3[GgxQTZ2N{[1OC=>
N1E-115 MlP2SpVv[3Srb36gRZN{[Xl? Mlv1NVAh|ryP MUCyJIg> M4fyR2ROW09? NFnyVoNKdmirYnn0d{B1cGViYYPz[Y1jdHlib3[gcYlkem:2dXL1cIV{KGGwZDDpcpRmem2nZHnheIUh\mmuYX3lcpR{KHSxIH\vdo0h\Xi2ZX7k[YQheHKxY3Xzd4V{ NWPLUlg4QTZ2N{[1OC=>
HeLa NFL6e|RHfW6ldHnvckBCe3OjeR?= M3ixc|ExKM7:TR?= NWn2dodLOzBibXnu M3\6R2lvcGmkaYTzJJRp\SCob4LtZZRqd25ib3[gd5Rz\XO|IH\pZoVzeyCjbnSgeIhmKGG|c3XtZox6KG:oII\pcoN2dGmwLXPvcpRicW6rbneg[o9k[WxiYXTo[ZNqd26| NVnQSlgyQTZ4OEC3Ni=>
CCL39 NGS2fZFHfW6ldHnvckBCe3OjeR?= NHrYR2Y{OCEQvF2= NFPIUnU{OCCvaX6= M4fwXGNwdXCuZYTlcJkh[WKxbHnzbIV{KGGldHn2ZZRqd25ib3[gUoEuUCCneHPoZY5o\XJiTljFNUBjgSCrboTl[5JqdnN? MmjiPVY6OzN6Mh?=
Mesothelial cells from rat mesentery NWPOVXRCUW64YYPpeoUhSXO|YYm= NYDYUnQyOzBizszN MnruNlAhcA>? NXvNcXEzSmyxY3vzJIlvfmG|aY\lJIFkfGm4aYT5 M2TSTVk6OzB6N{K=
NIH3T3 MnTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTTVlIyOCEQvF2= NH6zRmsyQCCm M4\u[2Rw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> MXqxNFAzOTN6Nh?=
Dbl-d M4nrRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXaNVAh|ryP NVvOV5NNOThiZB?= MXHTeJJwdmeueTDpcohq[mm2czDj[YxtKGe{b4f0bC=> Ml3HNVAxOjF|OE[=
Dbl-e MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU[xNEDPxE1? MmW0NVgh\A>? MljqUY9l\XKjdHXsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NUfNWYhQOTByMkGzPFY>
mNET1-d MlKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTYNVAh|ryP NYDHW|FTOThiZB?= MkWzV5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NUPjWXpLOTByMkGzPFY>
mNET1-e MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWixNEDPxE1? M4KyWVE5KGR? NYLwWWh1W3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh? NF7ad4QyODB{MUO4Oi=>
Ras-2 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnme5IyOCEQvF2= MkHTNVgh\A>? M3fFdnN1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp Ml\LNVAxOjF|OE[=
Ras-4 NF25bmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFr3TnMyOCEQvF2= M3H0fVE5KGR? NEPTW4tUfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NV;ad2dNOTByMkGzPFY>
Src-1 NXHMZnR1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvsVHEyOCEQvF2= NGLINGcyQCCm NH\zeZdFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp NWTQOmUzOTByMkGzPFY>
Src-4 Ml36S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFOzUVEyOCEQvF2= NET5eVQyQCCm M134b2Rw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> MkXtNVAxOjF|OE[=
NIH3T3 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVmxNEDPxE1? Mlz2NVgh\A>? NV3SOJk4TG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? NH7WU3YyODB{MUO4Oi=>
Src-1 NGfRcZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HMSVExKM7:TR?= MYexPEBl M{XwR2Rw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> NXLLUph2OTByMkGzPFY>
Src-2 MlnFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoP4NVAh|ryP NEOyNHAyQCCm MWjEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To MXuxNFAzOTN6Nh?=
SW620 NVLzS3dRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVOxNEDPxE1? MoHoNVgh\A>? M3\jeWRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> M3K3R|ExODJzM{i2
HCT15 NYDsRXBlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3iXlEyOCEQvF2= MV2xPEBl NID4cZNFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp M1\KUVExODJzM{i2
HCT116 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3z1[lExKM7:TR?= NWPBSohOOThiZB?= MXrTeJJwdmeueTDpcohq[mm2czDj[YxtKGe{b4f0bC=> NXTKfW45OTByMkGzPFY>
LS174T MnPYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3L6[VExKM7:TR?= MYCxPEBl MYrNc4RmemG2ZXz5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp NWGzdmIzOTByMkGzPFY>
Neonatal rat ventricular myocytes M3LuT2Z2dmO2aX;uJGF{e2G7 M2\qPFExKM7:TR?= MlLZOFghcA>? M1LISGlvcGmkaYTzJGVVNTFvaX7keYNm\CCrbnPy[YF{\XNiaX6gdJJwfGWrbjDzfY51cGW|aYOsJINmdGxic3n6[UBidmRibYnv[oljemmubHHyJI9z\2GwaYrheIlwdg>? NHKwdlUyODN6Nk[xNy=>
Stellate Cell MYPGeY5kfGmxbjDBd5NigQ>? MkXWNlUh|ryP MVexOUBucW5? NXHWeWdNUW6qaXLpeJMh\m:{bXH0bY9vKG:oIF[tZYN1cW5ic4Ty[ZN{KG[rYnXyd{BidmRicHjvd5Bpd3K7bHH0bY9vKG:oIH35c5NqdiCuaXfoeEBkcGGrbh?= NXXZZWFsOTB4MEC0PVY>
Rat Vascular Smooth Muscle Cells NWHYZWpNTnWwY4Tpc44hSXO|YYm= NHXOWZMyOCEQvF2= NILuUHczKGh? MVPJcohq[mm2czDhcodqd3SnboPpckBKUS2rbnT1Z4VlKGi7cHXyeJJweGi7 MlO1NVA3PDJ|MUe=
PC3 NXLPeI5NTnWwY4Tpc44hSXO|YYm= NE\OclkzPSEQvF2= MmWyNUBp MVLJcoR2[2W|IH3vdpBpd2yxZ3njZYwh[2ijbnfldy=> NUL4c2c6OTB5MkC0O|E>
PC3 MXXNbYdz[XSrb36gRZN{[Xl? M2LRcFI2KM7:TR?= NXPUWnhGOSCq MnjmTY5pcWKrdIOgeIhmKEKPRlKtR20h[W6mIITo[UBGT0Zvc4TpcZVt[XSnZDDtbYdz[XSrb36= NEXGb|MyODd{MES3NS=>
PC3 NUjteHFvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fKNVI2KM7:TR?= MnmwNVchcA>? NFzXTFZFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp NViySnNROTB5MkC0O|E>
LNCaP NUTFN5VTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTMcJdOOjVizszN NW\TPGliOTdiaB?= MXvEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To MojlNVA4OjB2N{G=
Rat hepatic stellate cells MVzGeY5kfGmxbjDBd5NigQ>? MV2zNEDPxE1? M3W0dlQ5KGh? MWDEbY1qdmm|aHXzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRYLrNkwh[W6mIHTlZ5Jm[XOnczDu[ZchTE6DIIP5cpRp\XOrcx?= M2PqbFExQDR3Nk[z
Pancreatic acinar cells MlLESpVv[3Srb36gRZN{[Xl? NV24[YJMOTEEoN88US=> MnXhO|AhdWmw NXW4[GJmWG:2ZX70bYF1\XNiQ1PLMZN1cW23bHH0[YQheGGwY4LlZZRq[yCnbor5cYUhe2WlcnX0bY9v NFHQenYyOjd2NUC4NC=>
C2C12 MV\GeY5kfGmxbjDBd5NigQ>? MYmxNOKh|ryP M4nCPFYhcA>? MYjQdoV3\W62czD0bIUhe2W{aX7lJJBpd3OyaH;yfYxifGmxbjDv[kBKWlNvMTDpcoR2[2WmIHL5JIlve3WuaX6gZY5lN2:{IGTOSk3PuQ>? NEn0[5UyPjJ4N{GyOC=>
PC 12 NIPzV3NHfW6ldHnvckBCe3OjeR?= Mli3NVDDqM7:TR?= NF3VcGczPCCq NF7FcHlCfHSnboXheIV{KGOjdHXjbI9t[W2rbnWgZolwe3mwdHjld4l{ MnnSNVYzOTl2MkS=
Cynomolgus monkey embryonic stem cells M1vVT2N6fG:2b4jpZ{BCe3OjeR?= M2PlSlIxKML3TR?= Mkj4NlQhcA>? MVXQdo9ud3SnczDjfWVUKGOnbHygd5Vzfmm4YXy= MoDtNVg6PDB6NUW=
TSGH 8301 NFztcYFOcWe{YYTpc44hSXO|YYm= MVSyNEDDvU1? NFjYZXoyKGh? NIfQTJdKdmO{ZXHz[ZMh[2WubDDtbYdz[XSrb36= NUKwS3ZqOTl6OU[0O|U>
Swiss3T3 M2mwbGNwdG:weT3mc5JucW6pIFHzd4F6 MXmxNEDDvU1? M2njSFE{KGR? NV[1VIpNUW6lcnXhd4V{KHC{b4P0ZZRmKGOnbHygZ49td267LX\vdo1qdmdiYXP0bZZqfHl? NIPReGMzOTR4NEmwNi=>
HT22 NVTGdmFqS3m2b4TvfIlkKEG|c3H5 MX[xNEDDvU1? NXLRRYozOTNiaB?= MoTOVJJwfGWldIOgZYdicW6|dDDncJV1[W2jdHWtbY5lfWOnZDDu[ZVzd26jbDDk[YF1cA>? NHX2b|AzOjhzMEizOS=>
Salivary gland stem cells NIHjR5BHfW6ldHnvckBCe3OjeR?= MnPkNVAhyrWP MWO3JIQ> MVHS[YR2[2W|IGPHV2Mhe2WwZYPj[Y5k\Q>? MVOyOVgxPDV4MB?=

... 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 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 64 mg/mL warming (199.83 mM)
Water 14 mg/mL (43.71 mM)
Ethanol <1 mg/mL
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

文献中の引用 (45)

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.

技術サポート&よくある質問(FAQ)

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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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