Y-27632 2HCl

Y-27632 2HClは一種の選択性的なROCK1 (p160ROCK)阻害剤で、無細胞試験でKi値が140 nMですが、ROCK1に作用する選択性は他のキナーゼ(PKC、cAMP依頼性タンパク質キナーゼ、,MLCKとPAKを含める)に作用する選択性より200倍以上が高くなります。

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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は一種の選択性的なROCK1 (p160ROCK)阻害剤で、無細胞試験でKi値が140 nMですが、ROCK1に作用する選択性は他のキナーゼ(PKC、cAMP依頼性タンパク質キナーゼ、,MLCKとPAKを含める)に作用する選択性より200倍以上が高くなります。
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 NGXDcpRHfW6ldHnvckBCe3OjeR?= MlrFNVAh|ryP NGXJflkzKGh? MlnXSG1UVw>? M17abGlvcGmkaYTzJJRp\SCjc4PlcYJtgSCxZjDtbYNzd3S3YoXs[ZMh[W6mIHnueIVzdWWmaXH0[UBncWyjbXXueJMhfG9iZn;ycUBmgHSnbnTl[EBxem:lZYPz[ZM> NHHiPIM6PjR5NkW0
N1E-115 MX\GeY5kfGmxbjDBd5NigQ>? MU[xNEDPxE1? NXjiTYtCOiCq M2PsdmROW09? MWLJcohq[mm2czD0bIUh[XO|ZX3icJkhd2ZibXnjdo91fWK3bHXzJIFv\CCrboTldo1m\GmjdHWg[olt[W2nboTzJJRwKG[xcn2g[Zh1\W6mZXSgdJJw[2W|c3Xz M3ji[|k3PDd4NUS=
HeLa MmPOSpVv[3Srb36gRZN{[Xl? NUXIenVyOTBizszN M2jPeFMxKG2rbh?= MWfJcohq[mm2czD0bIUh\m:{bXH0bY9vKG:oIIP0doV{eyCoaXLldpMh[W6mIITo[UBie3OnbXLsfUBw\iC4aX7jeYxqdi2lb370ZYlvcW6pIH\vZ4FtKGGmaHXzbY9vew>? NIO3bHU6PjZ6MEey
CCL39 NFT0UXVHfW6ldHnvckBCe3OjeR?= M1TSTlMxKM7:TR?= NFLPfGk{OCCvaX6= MVvDc41xdGW2ZXz5JIFjd2yrc3jld{Bi[3SrdnH0bY9vKG:oIF7hMWgh\XilaHHu[4VzKE6KRUGgZpkhcW62ZXfybY5{ NH;s[mk6Pjl|M{iy
Mesothelial cells from rat mesentery NFLDO41Kdn[jc3n2[UBCe3OjeR?= NITNOII{OCEQvF2= NUXZW2pnOjBiaB?= NUDDeWQySmyxY3vzJIlvfmG|aY\lJIFkfGm4aYT5 M1rPRlk6OzB6N{K=
NIH3T3 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7ySVMyOCEQvF2= NYfDOGx[OThiZB?= NEjTXHVFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp MmLVNVAxOjF|OE[=
Dbl-d M2e2bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY[xNEDPxE1? MXixPEBl NFG5V|hUfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MkjYNVAxOjF|OE[=
Dbl-e MlfLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHJUY0yOCEQvF2= M2DaPFE5KGR? NE\vd3lOd2SncnH0[Yx6KGmwaHnibZR{KGOnbHyg[5Jwf3Sq M2\t[FExODJzM{i2
mNET1-d M{fJOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDLNVAh|ryP M3v0T|E5KGR? M4GxO3N1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp MYmxNFAzOTN6Nh?=
mNET1-e NYfpTIwzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4n6NFExKM7:TR?= NFzYZ5UyQCCm NHPkOY9UfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NHrGWIkyODB{MUO4Oi=>
Ras-2 NV;CVI1uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37jOFExKM7:TR?= Mm\hNVgh\A>? MWPTeJJwdmeueTDpcohq[mm2czDj[YxtKGe{b4f0bC=> MVyxNFAzOTN6Nh?=
Ras-4 M2KzVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYKxNEDPxE1? M3HHU|E5KGR? MVPTeJJwdmeueTDpcohq[mm2czDj[YxtKGe{b4f0bC=> NUDQWYVMOTByMkGzPFY>
Src-1 NFnMcXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1ryfVExKM7:TR?= Ml;SNVgh\A>? M2rQTGRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> NFOwelAyODB{MUO4Oi=>
Src-4 M2jvWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7TNVAh|ryP M4jHblE5KGR? M2HzO2Rw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> MYixNFAzOTN6Nh?=
NIH3T3 M{TORmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17KOFExKM7:TR?= NXTPOoZVOThiZB?= M3LjdmRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> MUGxNFAzOTN6Nh?=
Src-1 NVz5fGdkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;CU2I3OTBizszN NIDPXooyQCCm MWLEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To MnPqNVAxOjF|OE[=
Src-2 M4\lO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1S4XFExKM7:TR?= Mn7GNVgh\A>? M2r6TmRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> NHH4eHYyODB{MUO4Oi=>
SW620 NUTJcogzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXhcmhOOTBizszN MoHKNVgh\A>? MYDEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To MX:xNFAzOTN6Nh?=
HCT15 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XTXVExKM7:TR?= NIrxZZoyQCCm M2XKPGRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> NV7k[5pMOTByMkGzPFY>
HCT116 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;WOFExKM7:TR?= NVvOcG05OThiZB?= MX;TeJJwdmeueTDpcohq[mm2czDj[YxtKGe{b4f0bC=> MXixNFAzOTN6Nh?=
LS174T MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELydGIyOCEQvF2= MWOxPEBl M{XjPG1w\GW{YYTlcJkhcW6qaXLpeJMh[2WubDDndo94fGh? NWLWOYppOTByMkGzPFY>
Neonatal rat ventricular myocytes Mo\RSpVv[3Srb36gRZN{[Xl? NG\jfWsyOCEQvF2= NHnVd|E1QCCq NFLXPFdKdmirYnn0d{BGXC1zLXnu[JVk\WRiaX7jdoVie2W|IHnuJJBzd3SnaX6gd5lvfGinc3nzMEBk\WyuIIPpfoUh[W6mIH35c4Zq[nKrbHzhdkBwemejbnn6ZZRqd25? NIfUd3YyODN6Nk[xNy=>
Stellate Cell MWnGeY5kfGmxbjDBd5NigQ>? MV[yOUDPxE1? MoX4NVUhdWmw NXTpUpNIUW6qaXLpeJMh\m:{bXH0bY9vKG:oIF[tZYN1cW5ic4Ty[ZN{KG[rYnXyd{BidmRicHjvd5Bpd3K7bHH0bY9vKG:oIH35c5NqdiCuaXfoeEBkcGGrbh?= NUXEZ5NrOTB4MEC0PVY>
Rat Vascular Smooth Muscle Cells M13IN2Z2dmO2aX;uJGF{e2G7 MkjBNVAh|ryP NVvUN4oxOiCq MYXJcohq[mm2czDhcodqd3SnboPpckBKUS2rbnT1Z4VlKGi7cHXyeJJweGi7 M1nJOVExPjR{M{G3
PC3 MknRSpVv[3Srb36gRZN{[Xl? MUCyOUDPxE1? NUjYV4ZrOSCq NHrlNWhKdmS3Y3XzJI1wenCqb3zv[4lk[WxiY3jhcodmew>? NHmwRowyODd{MES3NS=>
PC3 M1jYOm1q\3KjdHnvckBCe3OjeR?= NYnZXFRzOjVizszN NFjkfnEyKGh? MWfJcohq[mm2czD0bIUhSk2IQj3DUUBidmRidHjlJGVITi2|dHnteYxifGWmIH3p[5JifGmxbh?= MXKxNFczODR5MR?=
PC3 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUCyOUDPxE1? NI\kPW8yPyCq M3rZXmRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> MYmxNFczODR5MR?=
LNCaP NV[zOGRrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rBT|I2KM7:TR?= NFzqOHMyPyCq MY\Ec4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To NUjMeVZxOTB5MkC0O|E>
Rat hepatic stellate cells MYnGeY5kfGmxbjDBd5NigQ>? Mn;yN|Ah|ryP MlnuOFghcA>? MUDEbY1qdmm|aHXzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRYLrNkwh[W6mIHTlZ5Jm[XOnczDu[ZchTE6DIIP5cpRp\XOrcx?= MWGxNFg1PTZ4Mx?=
Pancreatic acinar cells MXHGeY5kfGmxbjDBd5NigQ>? MYexNOKh|ryP MnjSO|AhdWmw MWDQc5RmdnSrYYTld{BES0tvc4TpcZVt[XSnZDDwZY5kemWjdHnjJIVvgnmvZTDz[YNz\XSrb36= NG\ObXcyOjd2NUC4NC=>
C2C12 MmDESpVv[3Srb36gRZN{[Xl? MlPaNVDDqM7:TR?= M2j4Z|YhcA>? Ml3hVJJmfmWwdIOgeIhmKHOncnnu[UBxcG:|cHjvdplt[XSrb36gc4YhUVKVLUGgbY5lfWOnZDDifUBqdnO3bHnuJIFv\C:xcjDUUmYu|rF? M13JZlE3OjZ5MUK0
PC 12 MonDSpVv[3Srb36gRZN{[Xl? M1znOVExyqEQvF2= NYH1Zmp7OjRiaB?= MVzBeJRmdnWjdHXzJINifGWlaH;sZY1qdmViYnnvd5lvfGinc3nz NVe2cXBGOTZ{MUm0NlQ>
Cynomolgus monkey embryonic stem cells MlnVR5l1d3SxeHnjJGF{e2G7 Ml3oNlAhyrWP NXPKNlhlOjRiaB?= MnHTVJJwdW:2ZYOgZ5lGWyClZXzsJJN2en[rdnHs NHzVZ|MyQDl2MEi1OS=>
TSGH 8301 NGnleGFOcWe{YYTpc44hSXO|YYm= MViyNEDDvU1? NFH0NWsyKGh? MlfETY5kemWjc3XzJINmdGxibXnndoF1cW:w MlzaNVk5QTZ2N{W=
Swiss3T3 NWLGe|hPS2:ub375MYZwem2rbnegRZN{[Xl? NH;LXFAyOCEEtV2= NGnofHMyOyCm MX3JcoNz\WG|ZYOgdJJwe3SjdHWgZ4VtdCClb3zvcpku\m:{bXnu[{Bi[3Srdnn0fS=> M{nTPVIyPDZ2OUCy
HT22 NYq3V|VyS3m2b4TvfIlkKEG|c3H5 MkL5NVAhyrWP MlrYNVMhcA>? Mn3JVJJwfGWldIOgZYdicW6|dDDncJV1[W2jdHWtbY5lfWOnZDDu[ZVzd26jbDDk[YF1cA>? M174N|IzQDFyOEO1
Salivary gland stem cells NEDqOWlHfW6ldHnvckBCe3OjeR?= NEP2bYQyOCEEtV2= M4rpe|ch\A>? NIT1XI5T\WS3Y3XzJHNIW0Nic3Xu[ZNk\W6lZR?= M1XjOlI2QDB2NU[w

... 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 (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.

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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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