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 DescriptionPMID
Swiss 3T3 cells MYrGeY5kfGmxbjDBd5NigQ>? M2PtZ|ExKM7:TR?= MXGyJIg> MYLEUXNQ NFfIdJlKdmirYnn0d{B1cGViYYPz[Y1jdHlib3[gcYlkem:2dXL1cIV{KGGwZDDpcpRmem2nZHnheIUh\mmuYX3lcpR{KHSxIH\vdo0h\Xi2ZX7k[YQheHKxY3Xzd4V{ M3fKWVk3PDd4NUS=
N1E-115 NIDLfm5HfW6ldHnvckBCe3OjeR?= NUDBd4t7OTBizszN MWCyJIg> MWLEUXNQ MkDMTY5pcWKrdIOgeIhmKGG|c3XtZox6KG:oIH3pZ5JwfHWkdXzld{BidmRiaX70[ZJu\WSrYYTlJIZqdGGvZX70d{B1dyCob4LtJIV5fGWwZHXkJJBzd2Onc4Pldy=> M1\iOlk3PDd4NUS=
HeLa NETNW2VHfW6ldHnvckBCe3OjeR?= MlHZNVAh|ryP MmOwN|AhdWmw M4jvb2lvcGmkaYTzJJRp\SCob4LtZZRqd25ib3[gd5Rz\XO|IH\pZoVzeyCjbnSgeIhmKGG|c3XtZox6KG:oII\pcoN2dGmwLXPvcpRicW6rbneg[o9k[WxiYXTo[ZNqd26| M1GzZVk3PjhyN{K=
CCL39 NF2yZ5ZHfW6ldHnvckBCe3OjeR?= MXyzNEDPxE1? NYS3cWZFOzBibXnu MWjDc41xdGW2ZXz5JIFjd2yrc3jld{Bi[3SrdnH0bY9vKG:oIF7hMWgh\XilaHHu[4VzKE6KRUGgZpkhcW62ZXfybY5{ NVzGb5NuQTZ7M{O4Ni=>
Mesothelial cells from rat mesentery NXHGOWJxUW64YYPpeoUhSXO|YYm= MWizNEDPxE1? NFexbmkzOCCq MmfHRoxw[2u|IHnueoF{cX[nIHHjeIl3cXS7 M{PJUlk6OzB6N{K=
NIH3T3 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nQ[|ExKM7:TR?= NVTYTmZWOThiZB?= NHKxeIpFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp M1SyeVExODJzM{i2
Dbl-d NEP2[ItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETrSXkyOCEQvF2= M1;JcVE5KGR? MUDTeJJwdmeueTDpcohq[mm2czDj[YxtKGe{b4f0bC=> NYThVIZkOTByMkGzPFY>
Dbl-e MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXuxNEDPxE1? M2XlbVE5KGR? NF7hSlJOd2SncnH0[Yx6KGmwaHnibZR{KGOnbHyg[5Jwf3Sq MYOxNFAzOTN6Nh?=
mNET1-d M{PsR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M323U|ExKM7:TR?= NHLWbmEyQCCm NWfxTYE6W3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh? MYixNFAzOTN6Nh?=
mNET1-e NGDGSVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjzdIRlOTBizszN MkPpNVgh\A>? MnTpV5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg> M4X5flExODJzM{i2
Ras-2 NHzXTm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\2SZhbOTBizszN M2SzXlE5KGR? M2frb3N1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp M1yzO|ExODJzM{i2
Ras-4 NWnLNIN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXyNVAh|ryP M12zclE5KGR? MW\TeJJwdmeueTDpcohq[mm2czDj[YxtKGe{b4f0bC=> M1fxT|ExODJzM{i2
Src-1 NWXtcI5YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFj0SmcyOCEQvF2= NWDJbWRqOThiZB?= MkDISI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> M3fBXVExODJzM{i2
Src-4 NYrtVXprT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXyxNEDPxE1? NYjqWmNtOThiZB?= NED3WXlFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp NF3qUm0yODB{MUO4Oi=>
NIH3T3 M4LuRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLCTZEyOCEQvF2= NWLscmE6OThiZB?= NV\kNlFiTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? NX7C[JhCOTByMkGzPFY>
Src-1 NYO1V5ZGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVWxNEDPxE1? MXqxPEBl Mn[zSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> NWjLTlhXOTByMkGzPFY>
Src-2 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfMWlMyOCEQvF2= MorkNVgh\A>? NVu4[mxLTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? NUjCWJR2OTByMkGzPFY>
SW620 MnvLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DsNVExKM7:TR?= MWCxPEBl M1PXS2Rw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> MnvwNVAxOjF|OE[=
HCT15 M4TjR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjHXooxOTBizszN MkLMNVgh\A>? NX3MU2lxTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? MkLwNVAxOjF|OE[=
HCT116 NY\aR3hGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1qzXVExKM7:TR?= NEXWO5YyQCCm Mnj2V5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MYWxNFAzOTN6Nh?=
LS174T MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEP3[YUyOCEQvF2= MoLyNVgh\A>? MoLzUY9l\XKjdHXsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MoPRNVAxOjF|OE[=
Neonatal rat ventricular myocytes NGj2b4FHfW6ldHnvckBCe3OjeR?= NWDFNZNPOTBizszN NXXNO5VDPDhiaB?= M1zvN2lvcGmkaYTzJGVVNTFvaX7keYNm\CCrbnPy[YF{\XNiaX6gdJJwfGWrbjDzfY51cGW|aYOsJINmdGxic3n6[UBidmRibYnv[oljemmubHHyJI9z\2GwaYrheIlwdg>? M{HJclExOzh4NkGz
Stellate Cell MkGySpVv[3Srb36gRZN{[Xl? MXGyOUDPxE1? NUnjRYFkOTVibXnu NXrFdpVoUW6qaXLpeJMh\m:{bXH0bY9vKG:oIF[tZYN1cW5ic4Ty[ZN{KG[rYnXyd{BidmRicHjvd5Bpd3K7bHH0bY9vKG:oIH35c5NqdiCuaXfoeEBkcGGrbh?= NYXpR4FbOTB4MEC0PVY>
Rat Vascular Smooth Muscle Cells MUjGeY5kfGmxbjDBd5NigQ>? MVKxNEDPxE1? MWqyJIg> Ml7aTY5pcWKrdIOgZY5ocW:2ZX7zbY4hUUlvaX7keYNm\CCqeYDldpRzd3CqeR?= MnLuNVA3PDJ|MUe=
PC3 MXrGeY5kfGmxbjDBd5NigQ>? Mlv6NlUh|ryP MWCxJIg> NVvFTJB3UW6mdXPld{Bud3KyaH;sc4dq[2GuIHPoZY5o\XN? M{TGOVExPzJyNEex
PC3 NEfFSpdOcWe{YYTpc44hSXO|YYm= M{HMWlI2KM7:TR?= NX7uTG9HOSCq NE\nPHdKdmirYnn0d{B1cGViQl3GRk1EVSCjbnSgeIhmKEWJRj3zeIlufWyjdHXkJI1q\3KjdHnvci=> MoPKNVA4OjB2N{G=
PC3 MnW4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MViyOUDPxE1? NHjVblYyPyCq NYPzVFJZTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? NFXUdpIyODd{MES3NS=>
LNCaP MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEi5UWkzPSEQvF2= NUjP[WI{OTdiaB?= NHWyRVdFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp NF3mZ3QyODd{MES3NS=>
Rat hepatic stellate cells MVLGeY5kfGmxbjDBd5NigQ>? NELMSXk{OCEQvF2= NHPzcFA1QCCq NIDHc|JFcW2rbnnzbIV{KHSqZTDwbI9{eGixconsZZRqd25ib3[gSZJsOixiYX7kJIRm[3KnYYPld{Bv\XdiRF7BJJN6dnSqZYPpdy=> NYrQ[JB6OTB6NEW2OlM>
Pancreatic acinar cells MUnGeY5kfGmxbjDBd5NigQ>? NGLmemoyOMLizszN NX7F[2Q2PzBibXnu NVfLfWROWG:2ZX70bYF1\XNiQ1PLMZN1cW23bHH0[YQheGGwY4LlZZRq[yCnbor5cYUhe2WlcnX0bY9v NGH4[YEyOjd2NUC4NC=>
C2C12 M3\KWGZ2dmO2aX;uJGF{e2G7 NYrYb4tpOTEEoN88US=> MnTzOkBp NITyTZhRemW4ZX70d{B1cGVic3XybY5mKHCqb4PwbI9zgWyjdHnvckBw\iCLUmOtNUBqdmS3Y3XkJIJ6KGmwc4XsbY4h[W6mL3;yJHRPTi4QsR?= NUfpbYNSOTZ{NkexNlQ>
PC 12 M1vM[GZ2dmO2aX;uJGF{e2G7 MXixNOKh|ryP NW\OR3ZlOjRiaB?= NGDOXmtCfHSnboXheIV{KGOjdHXjbI9t[W2rbnWgZolwe3mwdHjld4l{ NUDpSGF1OTZ{MUm0NlQ>
Cynomolgus monkey embryonic stem cells MkLsR5l1d3SxeHnjJGF{e2G7 NVSySFNNOjBiwsXN M4\jbFI1KGh? MXHQdo9ud3SnczDjfWVUKGOnbHygd5Vzfmm4YXy= MVKxPFk1ODh3NR?=
TSGH 8301 M1\uOG1q\3KjdHnvckBCe3OjeR?= NG\OOWszOCEEtV2= MlLONUBp NVH5fmJUUW6lcnXhd4V{KGOnbHygcYloemG2aX;u NEf2eVcyQTh7NkS3OS=>
Swiss3T3 NHzYN5REd2yxbomt[o9zdWmwZzDBd5NigQ>? MVyxNEDDvU1? MYGxN{Bl MnjJTY5kemWjc3XzJJBzd3O2YYTlJINmdGxiY3;sc456NW[xcn3pcoch[WO2aY\peJk> MmnHNlE1PjR7MEK=
HT22 NVWwd2xSS3m2b4TvfIlkKEG|c3H5 Mo\ZNVAhyrWP MVWxN{Bp M3v1XnBzd3SnY4TzJIFo[Wmwc4Sg[4x2fGGvYYTlMYlv\HWlZXSgcoV2em:wYXyg[IVifGh? MnTqNlI5OTB6M{W=
Salivary gland stem cells M3zweWZ2dmO2aX;uJGF{e2G7 MVWxNEDDvU1? M3vqblch\A>? MoXZVoVlfWOnczDTS3NEKHOnbnXzZ4Vv[2V? MYKyOVgxPDV4MB?=

... 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 (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.

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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