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 NEn5SYZHfW6ldHnvckBCe3OjeR?= MlviNVAh|ryP NUH3OHJsOiCq NFzHOJpFVVOR M2jqXGlvcGmkaYTzJJRp\SCjc4PlcYJtgSCxZjDtbYNzd3S3YoXs[ZMh[W6mIHnueIVzdWWmaXH0[UBncWyjbXXueJMhfG9iZn;ycUBmgHSnbnTl[EBxem:lZYPz[ZM> MYG5OlQ4PjV2
N1E-115 M{jFU2Z2dmO2aX;uJGF{e2G7 M2j2TFExKM7:TR?= NGPNXmszKGh? NX\OSHFyTE2VTx?= NWfQWYdnUW6qaXLpeJMhfGinIHHzd4Vu[my7IH;mJI1q[3KxdIXieYxmeyCjbnSgbY51\XKvZXTpZZRmKG[rbHHt[Y51eyC2bzDmc5JuKGW6dHXu[IVlKHC{b3Pld5Nmew>? M{DJU|k3PDd4NUS=
HeLa NEi1PHpHfW6ldHnvckBCe3OjeR?= M3j3d|ExKM7:TR?= MWCzNEBucW5? MY\Jcohq[mm2czD0bIUh\m:{bXH0bY9vKG:oIIP0doV{eyCoaXLldpMh[W6mIITo[UBie3OnbXLsfUBw\iC4aX7jeYxqdi2lb370ZYlvcW6pIH\vZ4FtKGGmaHXzbY9vew>? MVS5OlY5ODd{
CCL39 MVrGeY5kfGmxbjDBd5NigQ>? NWTxUIY3OzBizszN MnHSN|AhdWmw MoPhR49ueGyndHXsfUBi[m:uaYPo[ZMh[WO2aY\heIlwdiCxZjDOZU1JKGW6Y3jhcodmeiCQSFWxJIJ6KGmwdHXndolvew>? NFzXUlE6Pjl|M{iy
Mesothelial cells from rat mesentery MWjJcpZie2m4ZTDBd5NigQ>? Mn;vN|Ah|ryP NGruZpIzOCCq Mn74Roxw[2u|IHnueoF{cX[nIHHjeIl3cXS7 MlfpPVk{ODh5Mh?=
NIH3T3 M3O4RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnkTGYyOCEQvF2= MnjYNVgh\A>? Mmj1SI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> MljVNVAxOjF|OE[=
Dbl-d M{PJZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPsU|M2OTBizszN MlfCNVgh\A>? NHS1dJVUfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NEnHVJYyODB{MUO4Oi=>
Dbl-e NHvqb|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17lXFExKM7:TR?= MWexPEBl MlLVUY9l\XKjdHXsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MXexNFAzOTN6Nh?=
mNET1-d MknwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nGSFExKM7:TR?= NWDpXFZwOThiZB?= NYnlbWpNW3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh? M4joOFExODJzM{i2
mNET1-e NHrQTWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWWxNEDPxE1? MWWxPEBl MlKxV5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg> M{niVVExODJzM{i2
Ras-2 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DhTFExKM7:TR?= NWXlVlgzOThiZB?= MoTsV5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MYOxNFAzOTN6Nh?=
Ras-4 M1rSNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\r[24yOCEQvF2= M13M[lE5KGR? MVLTeJJwdmeueTDpcohq[mm2czDj[YxtKGe{b4f0bC=> NF7QTIgyODB{MUO4Oi=>
Src-1 MkXkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rUeVExKM7:TR?= MXuxPEBl MULEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To MYWxNFAzOTN6Nh?=
Src-4 M2XkSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVOxNEDPxE1? NFLLfXcyQCCm M4\Oe2Rw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> NFHMOZQyODB{MUO4Oi=>
NIH3T3 NV7Y[XRVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUL3OIdOOTBizszN Mk\SNVgh\A>? MlfhSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> MoKwNVAxOjF|OE[=
Src-1 Mn\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDaNVAh|ryP NXH2OFA{OThiZB?= NGLCdnFFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp NV\1fXFiOTByMkGzPFY>
Src-2 NX35Uok2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIj1e2MyOCEQvF2= NU\RS2t{OThiZB?= MorVSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> MnnONVAxOjF|OE[=
SW620 M{DuSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYW1WmdQOTBizszN MYmxPEBl NVrVO5dyTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? MkPZNVAxOjF|OE[=
HCT15 NFL5O|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfMNVAh|ryP MV:xPEBl NFXqeFNFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp MlroNVAxOjF|OE[=
HCT116 M1PuR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHTNVAh|ryP MWmxPEBl NHfqN|RUfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NHnaeVcyODB{MUO4Oi=>
LS174T MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWq3dI5lOTBizszN NF\C[Y0yQCCm Mn[3UY9l\XKjdHXsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? M4\BO|ExODJzM{i2
Neonatal rat ventricular myocytes NXXJ[HE6TnWwY4Tpc44hSXO|YYm= M17RVFExKM7:TR?= NVPLcI04PDhiaB?= Mn7CTY5pcWKrdIOgSXQuOS2rbnT1Z4VlKGmwY4LlZZNmeyCrbjDwdo91\WmwIIP5cpRp\XOrczygZ4VtdCC|aYrlJIFv\CCveX;mbYJzcWyuYYKgc5Jo[W6renH0bY9v NXzJ[pJHOTB|OE[2NVM>
Stellate Cell MoXUSpVv[3Srb36gRZN{[Xl? NXLEfnJwOjVizszN NFLHVJQyPSCvaX6= MlfzTY5pcWKrdIOg[o9zdWG2aX;uJI9nKEZvYXP0bY4he3S{ZYPzJIZq[mW{czDhcoQheGixc4Doc5J6dGG2aX;uJI9nKG27b4PpckBtcWeqdDDjbIFqdg>? Mn:4NVA3ODB2OU[=
Rat Vascular Smooth Muscle Cells NYe4T41ETnWwY4Tpc44hSXO|YYm= MUWxNEDPxE1? NF2zfJQzKGh? NYrxepJqUW6qaXLpeJMh[W6paX;0[Y5{cW5iSVmtbY5lfWOnZDDofZBmenS{b4DofS=> MYmxNFY1OjNzNx?=
PC3 M1XDdmZ2dmO2aX;uJGF{e2G7 NF3SeYQzPSEQvF2= MYOxJIg> MXHJcoR2[2W|IH3vdpBpd2yxZ3njZYwh[2ijbnfldy=> Mki5NVA4OjB2N{G=
PC3 NHvCNnJOcWe{YYTpc44hSXO|YYm= NGXOdWQzPSEQvF2= M3XO[VEhcA>? M2Sx[GlvcGmkaYTzJJRp\SCETV\CMWNOKGGwZDD0bIUhTUeILYP0bY12dGG2ZXSgcYloemG2aX;u NVLsOXhkOTB5MkC0O|E>
PC3 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;YNlUh|ryP NIXu[HQyPyCq MVXEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To NFfnfGwyODd{MES3NS=>
LNCaP NFLSbJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoezNlUh|ryP NYfSbmVpOTdiaB?= M33hbmRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> NUnnZ3dyOTB5MkC0O|E>
Rat hepatic stellate cells MUfGeY5kfGmxbjDBd5NigQ>? M{TOflMxKM7:TR?= NGjkcok1QCCq NHrTdGFFcW2rbnnzbIV{KHSqZTDwbI9{eGixconsZZRqd25ib3[gSZJsOixiYX7kJIRm[3KnYYPld{Bv\XdiRF7BJJN6dnSqZYPpdy=> M37LblExQDR3Nk[z
Pancreatic acinar cells MYDGeY5kfGmxbjDBd5NigQ>? MoD5NVDDqM7:TR?= MXu3NEBucW5? NHuw[FlRd3SnboTpZZRmeyCFQ1utd5RqdXWuYYTl[EBx[W6lcnXheIlkKGWweont[UB{\WO{ZYTpc44> Mn:zNVI4PDVyOEC=
C2C12 MX3GeY5kfGmxbjDBd5NigQ>? MmLDNVDDqM7:TR?= MYS2JIg> MoLPVJJmfmWwdIOgeIhmKHOncnnu[UBxcG:|cHjvdplt[XSrb36gc4YhUVKVLUGgbY5lfWOnZDDifUBqdnO3bHnuJIFv\C:xcjDUUmYu|rF? MkHKNVYzPjdzMkS=
PC 12 MnezSpVv[3Srb36gRZN{[Xl? Mnq3NVDDqM7:TR?= M17YV|I1KGh? NH\PZVNCfHSnboXheIV{KGOjdHXjbI9t[W2rbnWgZolwe3mwdHjld4l{ NYDuSnJCOTZ{MUm0NlQ>
Cynomolgus monkey embryonic stem cells NInZPHlEgXSxdH;4bYMhSXO|YYm= M4D3[FIxKML3TR?= M1\IUVI1KGh? M{fab3Bzd22xdHXzJIN6TVNiY3XscEB{fXK4aY\hcC=> MYWxPFk1ODh3NR?=
TSGH 8301 NFi3Z21OcWe{YYTpc44hSXO|YYm= NVHaU2tCOjBiwsXN NY\jfYp[OSCq NIi1[YtKdmO{ZXHz[ZMh[2WubDDtbYdz[XSrb36= NELjPIEyQTh7NkS3OS=>
Swiss3T3 NHi2[49Ed2yxbomt[o9zdWmwZzDBd5NigQ>? Mn\zNVAhyrWP M1r1WVE{KGR? NFvrUVdKdmO{ZXHz[ZMheHKxc4TheIUh[2WubDDjc4xwdnlvZn;ycYlv\yCjY4Tpeol1gQ>? NFW0OpIzOTR4NEmwNi=>
HT22 M{fpT2N6fG:2b4jpZ{BCe3OjeR?= NILTdosyOCEEtV2= NG\E[2QyOyCq NH6zRo5Rem:2ZXP0d{Bi\2GrboP0JIdtfXSjbXH0[U1qdmS3Y3XkJI5mfXKxbnHsJIRm[XSq MoPwNlI5OTB6M{W=
Salivary gland stem cells NF7VZnBHfW6ldHnvckBCe3OjeR?= NVnrO4hLOTBiwsXN Ml7UO{Bl NX:4N4pZWmWmdXPld{BUT1OFIIPlcoV{[2WwY3W= NF\wc2YzPThyNEW2NC=>

... 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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