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 MnfWSpVv[3Srb36gRZN{[Xl? Mlu5NVAh|ryP M4qyUVIhcA>? Mo\ESG1UVw>? MlXqTY5pcWKrdIOgeIhmKGG|c3XtZox6KG:oIH3pZ5JwfHWkdXzld{BidmRiaX70[ZJu\WSrYYTlJIZqdGGvZX70d{B1dyCob4LtJIV5fGWwZHXkJJBzd2Onc4Pldy=> NYj5dZptQTZ2N{[1OC=>
N1E-115 NUPiNXVHTnWwY4Tpc44hSXO|YYm= MnflNVAh|ryP M2DaW|IhcA>? MY\EUXNQ NH7PO|VKdmirYnn0d{B1cGViYYPz[Y1jdHlib3[gcYlkem:2dXL1cIV{KGGwZDDpcpRmem2nZHnheIUh\mmuYX3lcpR{KHSxIH\vdo0h\Xi2ZX7k[YQheHKxY3Xzd4V{ NYXpOYZMQTZ2N{[1OC=>
HeLa Mn7TSpVv[3Srb36gRZN{[Xl? Mom1NVAh|ryP NHvrUVc{OCCvaX6= NIrkU|FKdmirYnn0d{B1cGViZn;ycYF1cW:wIH;mJJN1emW|czDmbYJmenNiYX7kJJRp\SCjc4PlcYJtgSCxZjD2bY5kfWyrbj3jc451[WmwaX7nJIZw[2GuIHHkbIV{cW:wcx?= MoTFPVY3QDB5Mh?=
CCL39 NWf0cGlkTnWwY4Tpc44hSXO|YYm= NV3FbYw2OzBizszN MWCzNEBucW5? MWTDc41xdGW2ZXz5JIFjd2yrc3jld{Bi[3SrdnH0bY9vKG:oIF7hMWgh\XilaHHu[4VzKE6KRUGgZpkhcW62ZXfybY5{ M1PQW|k3QTN|OEK=
Mesothelial cells from rat mesentery NWrMO|JOUW64YYPpeoUhSXO|YYm= NVqzbVZTOzBizszN MWGyNEBp M3rafmJtd2OtczDpcpZie2m4ZTDhZ5Rqfmm2eR?= NEW0bVg6QTNyOEey
NIH3T3 M3nHbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnxNVAh|ryP MlvzNVgh\A>? NH:4WGpFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp MV:xNFAzOTN6Nh?=
Dbl-d M1PSXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknJNVAh|ryP MUmxPEBl MUXTeJJwdmeueTDpcohq[mm2czDj[YxtKGe{b4f0bC=> NXr1TpFvOTByMkGzPFY>
Dbl-e MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvqTYpkOTBizszN M{\4XFE5KGR? NXL6[FNkVW:mZYLheIVtgSCrbnjpZol1eyClZXzsJIdzd3e2aB?= MmLKNVAxOjF|OE[=
mNET1-d M{W2Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHu4[WIyOCEQvF2= MmPBNVgh\A>? NWThcVFVW3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh? M{Pz[|ExODJzM{i2
mNET1-e NFXHb3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHzNVAh|ryP MnvVNVgh\A>? MYnTeJJwdmeueTDpcohq[mm2czDj[YxtKGe{b4f0bC=> M1zySVExODJzM{i2
Ras-2 NF[1fVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fhO|ExKM7:TR?= NEe0UIoyQCCm NEjZSpFUfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NV20WW81OTByMkGzPFY>
Ras-4 M4rnTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTEUoRnOTBizszN M2f2WFE5KGR? MonpV5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg> M3LBZVExODJzM{i2
Src-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUWwW4NXOTBizszN NVjmZYpyOThiZB?= MnL3SI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> M2\OPVExODJzM{i2
Src-4 M4fyRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYixNEDPxE1? M1jYb|E5KGR? NYntZVczTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? MnT2NVAxOjF|OE[=
NIH3T3 M136eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmX2NVAh|ryP M{[3WlE5KGR? NHe2ellFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp NIO1XGIyODB{MUO4Oi=>
Src-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnlRXcyOCEQvF2= M3exelE5KGR? NISybXdFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp MXmxNFAzOTN6Nh?=
Src-2 MlG2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETIVGoyOCEQvF2= M2\PbVE5KGR? M4fWSmRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> NULWWYJsOTByMkGzPFY>
SW620 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnNNVAh|ryP NWHB[IExOThiZB?= NHrJRYFFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp NFXFOpoyODB{MUO4Oi=>
HCT15 NVLicHQ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmC5NVAh|ryP NV22WG5{OThiZB?= MXTEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To NEXWW|MyODB{MUO4Oi=>
HCT116 MnXVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnNNVAh|ryP MojaNVgh\A>? M2HXd3N1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp M{DYUVExODJzM{i2
LS174T MlrCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnabJAyOCEQvF2= M4DXRVE5KGR? NWfKWpFlVW:mZYLheIVtgSCrbnjpZol1eyClZXzsJIdzd3e2aB?= MWmxNFAzOTN6Nh?=
Neonatal rat ventricular myocytes MlGySpVv[3Srb36gRZN{[Xl? M{W2WlExKM7:TR?= NGDYTm81QCCq MWfJcohq[mm2czDFWE0yNWmwZIXj[YQhcW6lcnXhd4V{KGmwIIDyc5RmcW5ic4nueIhme2m|LDDj[YxtKHOrenWgZY5lKG27b3\pZpJqdGyjcjDvdodidmm8YYTpc44> NHfEdZIyODN6Nk[xNy=>
Stellate Cell MmDESpVv[3Srb36gRZN{[Xl? NVTZVnIzOjVizszN MkfCNVUhdWmw MV;Jcohq[mm2czDmc5Ju[XSrb36gc4YhTi2jY4TpckB{fHKnc4Og[olj\XK|IHHu[EBxcG:|cHjvdplt[XSrb36gc4YhdXmxc3nuJIxq\2i2IHPoZYlv NXrNb|h5OTB4MEC0PVY>
Rat Vascular Smooth Muscle Cells M2XXXGZ2dmO2aX;uJGF{e2G7 NUXGZldnOTBizszN MXiyJIg> M1PWS2lvcGmkaYTzJIFv\2mxdHXud4lvKEmLLXnu[JVk\WRiaInw[ZJ1em:yaIm= MXSxNFY1OjNzNx?=
PC3 MUXGeY5kfGmxbjDBd5NigQ>? NUjr[|k4OjVizszN MVexJIg> Mn7YTY5lfWOnczDtc5JxcG:ub3fpZ4FtKGOqYX7n[ZM> MnzkNVA4OjB2N{G=
PC3 M3r2V21q\3KjdHnvckBCe3OjeR?= M4fMTlI2KM7:TR?= NEfpfVgyKGh? M4TXU2lvcGmkaYTzJJRp\SCETV\CMWNOKGGwZDD0bIUhTUeILYP0bY12dGG2ZXSgcYloemG2aX;u Mn;pNVA4OjB2N{G=
PC3 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PqW|I2KM7:TR?= NIHoSGIyPyCq MnnXSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> NFnBR3QyODd{MES3NS=>
LNCaP NXrNTZV3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjjPXEzPSEQvF2= NFv1Z5YyPyCq NVHmSmk6TG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? M2\rZlExPzJyNEex
Rat hepatic stellate cells Mme5SpVv[3Srb36gRZN{[Xl? M3rqeFMxKM7:TR?= M3TKZlQ5KGh? M2\UUGRqdWmwaYPo[ZMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDFdoszNCCjbnSg[IVkemWjc3XzJI5mfyCGTlGgd5lvfGinc3nz NVviSGdDOTB6NEW2OlM>
Pancreatic acinar cells MlPkSpVv[3Srb36gRZN{[Xl? NYDTUnU{OTEEoN88US=> MnrIO|AhdWmw NHvoUVdRd3SnboTpZZRmeyCFQ1utd5RqdXWuYYTl[EBx[W6lcnXheIlkKGWweont[UB{\WO{ZYTpc44> MVWxNlc1PTB6MB?=
C2C12 NHTqZodHfW6ldHnvckBCe3OjeR?= MWSxNOKh|ryP M{L3c|YhcA>? MkfOVJJmfmWwdIOgeIhmKHOncnnu[UBxcG:|cHjvdplt[XSrb36gc4YhUVKVLUGgbY5lfWOnZDDifUBqdnO3bHnuJIFv\C:xcjDUUmYu|rF? NY\nZ|BOOTZ{NkexNlQ>
PC 12 NWnwSmh2TnWwY4Tpc44hSXO|YYm= NGXz[m0yOMLizszN M1zwUlI1KGh? NYe0NnN6SXS2ZX71ZZRmeyClYYTlZ4hwdGGvaX7lJIJqd3O7boTo[ZNqew>? M4m2R|E3OjF7NEK0
Cynomolgus monkey embryonic stem cells MlvyR5l1d3SxeHnjJGF{e2G7 NGC3ZW0zOCEEtV2= M1vMbFI1KGh? NUCwNGViWHKxbX;0[ZMh[3mHUzDj[YxtKHO3co\peoFt NYTye5Z4OTh7NEC4OVU>
TSGH 8301 NEjnc4JOcWe{YYTpc44hSXO|YYm= NV\yO3JROjBiwsXN NYr4cGdoOSCq MYXJcoNz\WG|ZYOgZ4VtdCCvaXfyZZRqd25? MXqxPVg6PjR5NR?=
Swiss3T3 NHrnTW9Ed2yxbomt[o9zdWmwZzDBd5NigQ>? NUe5TnlLOTBiwsXN M4\oWVE{KGR? MlLDTY5kemWjc3XzJJBzd3O2YYTlJINmdGxiY3;sc456NW[xcn3pcoch[WO2aY\peJk> NGLJfnAzOTR4NEmwNi=>
HT22 NVjTW3dyS3m2b4TvfIlkKEG|c3H5 MmCwNVAhyrWP MmXKNVMhcA>? M1HXOXBzd3SnY4TzJIFo[Wmwc4Sg[4x2fGGvYYTlMYlv\HWlZXSgcoV2em:wYXyg[IVifGh? M1H6b|IzQDFyOEO1
Salivary gland stem cells MVLGeY5kfGmxbjDBd5NigQ>? Ml;ONVAhyrWP Ml;CO{Bl MkTGVoVlfWOnczDTS3NEKHOnbnXzZ4Vv[2V? Mn;ONlU5ODR3NkC=

... 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

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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