Y-27632 2HCl

製品コードS1049

Y-27632 2HCl化学構造

分子量(MW):320.26

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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JPY 22462.12 あり
JPY 10079.16 あり
JPY 17278.56 あり
JPY 24477.96 あり
JPY 82073.16 あり

文献中の引用(46)

カスタマーフィードバック(5)

  • The ROCK inhibitors fasudil and Y27632 prevented SCP2 cell bone metastasis in nude mice (n = 10 per group). Shown are BLI images of bone metastases, IHC analyses of SMAD3 C-tail phosphorylation and PTHLH, osteoclast TRAP staining, and BLI quantitation.

    J Clin Invest, 2014, 124(4): 1646-59. Y-27632 2HCl purchased from Selleck.

    YAP nuclear localization in fibroblasts treated with PRP-Exos was blocked by Y-27632 2HCl. Scale bar: 50 μm.

    Theranostics, 2017, 7(1):81-96. Y-27632 2HCl purchased from Selleck.

  • The Rho GTPase-JNK pathway is required for the inhibitory effects of vandetanib on Calu-6 cells invasion. Calu-6 cells were incubated for 24 h in the presence or absence of vandetanib (1 or 2 uM), SP600125 (50 or 100 uM), and Y27632 (5 or 10 uM). The morphology of the Calu-6 cells was examined under a light microscope. Scale bar: 50 um.

    Mol Neurobiol 2015 10.1007/s12035-014-9084-z. Y-27632 2HCl purchased from Selleck.

    Effect of mechanical strain on cell morphology. (A) SEM analyses indicate that strain-induced cell elongation is prevented by treatment with HA1100 and Y27632. (B) Quantification of cellular area in the indicated conditions (n = 20). (C) F-actin staining of control, strained and HA1100 or Y27632-treated cells attests that inhibition of RhoA/ROCK prevents mechanical strain-induced cell elongation. *p < 0.05 compared to control without strain (CTL).

    J Mol Cell Cardiol 2014 67, 49-59. Y-27632 2HCl purchased from Selleck.

  • Dev Biol 2012 370, 33-41. Y-27632 2HCl purchased from Selleck.

製品安全説明書

ROCK阻害剤の選択性比較

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 (p160ROCK) [1]
(Cell-free assay)
ROCK2 [6]
(Cell-free assay)
140 nM(Ki) 300 nM(Ki)
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Swiss 3T3 cells NIL4PIVHfW6ldHnvckBCe3OjeR?= NVTyZWZIOTBizszN M{XUdlIhcA>? NEmyR|dFVVOR MXLJcohq[mm2czD0bIUh[XO|ZX3icJkhd2ZibXnjdo91fWK3bHXzJIFv\CCrboTldo1m\GmjdHWg[olt[W2nboTzJJRwKG[xcn2g[Zh1\W6mZXSgdJJw[2W|c3Xz NHTCNFk6PjR5NkW0
N1E-115 MX7GeY5kfGmxbjDBd5NigQ>? M1HLT|ExKM7:TR?= NE\4WIMzKGh? NHHTPWNFVVOR MYnJcohq[mm2czD0bIUh[XO|ZX3icJkhd2ZibXnjdo91fWK3bHXzJIFv\CCrboTldo1m\GmjdHWg[olt[W2nboTzJJRwKG[xcn2g[Zh1\W6mZXSgdJJw[2W|c3Xz MUi5OlQ4PjV2
HeLa MXHGeY5kfGmxbjDBd5NigQ>? NW\2d2FOOTBizszN MnTLN|AhdWmw MnPsTY5pcWKrdIOgeIhmKG[xcn3heIlwdiCxZjDzeJJme3NiZnni[ZJ{KGGwZDD0bIUh[XO|ZX3icJkhd2ZidnnuZ5VtcW5vY3;ueIFqdmmwZzDmc4NidCCjZHjld4lwdnN? MlfYPVY3QDB5Mh?=
CCL39 NXLE[W5uTnWwY4Tpc44hSXO|YYm= M3XK[FMxKM7:TR?= MWKzNEBucW5? MnLUR49ueGyndHXsfUBi[m:uaYPo[ZMh[WO2aY\heIlwdiCxZjDOZU1JKGW6Y3jhcodmeiCQSFWxJIJ6KGmwdHXndolvew>? MWK5Olk{Ozh{
Mesothelial cells from rat mesentery MXrJcpZie2m4ZTDBd5NigQ>? MljkN|Ah|ryP Mn3pNlAhcA>? NF6x[pVDdG:la4OgbY53[XOrdnWgZYN1cX[rdIm= NXLwcZZHQTl|MEi3Ni=>
NIH3T3 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjvWnYyOCEQvF2= NF7kZYMyQCCm Ml\pSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> M4PvV|ExODJzM{i2
Dbl-d MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjOVlAyOCEQvF2= MWGxPEBl MVvTeJJwdmeueTDpcohq[mm2czDj[YxtKGe{b4f0bC=> M3S4clExODJzM{i2
Dbl-e Moi2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Moe5NVAh|ryP NUHNbo1tOThiZB?= NFHBd2lOd2SncnH0[Yx6KGmwaHnibZR{KGOnbHyg[5Jwf3Sq NWrLbY0zOTByMkGzPFY>
mNET1-d Mk\KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7TNVAh|ryP NYnlS5VrOThiZB?= NXzsUVZbW3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh? NYnz[2ttOTByMkGzPFY>
mNET1-e M{XVV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXsNVAh|ryP NF7mPJQyQCCm M{XqW3N1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp NYWzPYxIOTByMkGzPFY>
Ras-2 M1vS[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfDWXoyOCEQvF2= MY[xPEBl M4C0SXN1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp MkDlNVAxOjF|OE[=
Ras-4 NVHnc5NsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7yUWJjOTBizszN NVfGUHd5OThiZB?= M3rWO3N1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp NWrvRnNlOTByMkGzPFY>
Src-1 MnriS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUSxNEDPxE1? MX:xPEBl MnyySI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> MnzBNVAxOjF|OE[=
Src-4 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXGxNEDPxE1? M1iwblE5KGR? MYnEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To NVXCOmVWOTByMkGzPFY>
NIH3T3 NXrrbpc5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXKxNEDPxE1? MoDXNVgh\A>? MnS1SI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> NU\hWJpsOTByMkGzPFY>
Src-1 M1nGc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfOdXZqOTBizszN MY[xPEBl MXLEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To NH;KU2kyODB{MUO4Oi=>
Src-2 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\6T2hEOTBizszN M2nHXlE5KGR? NF[3XFBFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp M2HySFExODJzM{i2
SW620 NFe5RXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUmzboNXOTBizszN NULpdFJbOThiZB?= NGPEWYpFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp M2XuSFExODJzM{i2
HCT15 NHH5T2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{X5fFExKM7:TR?= NUTodJFGOThiZB?= NWrkOXRNTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? NVvyelRtOTByMkGzPFY>
HCT116 NUW0OZBMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLuNVAh|ryP M2K5SFE5KGR? Mn7zV5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MXexNFAzOTN6Nh?=
LS174T NYPufoR7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHZNVAh|ryP MX6xPEBl MWnNc4RmemG2ZXz5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp NEfER5gyODB{MUO4Oi=>
Neonatal rat ventricular myocytes MmnDSpVv[3Srb36gRZN{[Xl? M1TWelExKM7:TR?= NVu2NWVTPDhiaB?= NUTG[XdvUW6qaXLpeJMhTVRvMT3pcoR2[2WmIHnuZ5Jm[XOnczDpckBxem:2ZXnuJJN6dnSqZYPpd{wh[2WubDDzbZpmKGGwZDDtfY9ncWK{aXzsZZIhd3KpYX7pfoF1cW:w NXTKWmtXOTB|OE[2NVM>
Stellate Cell M361R2Z2dmO2aX;uJGF{e2G7 MmGzNlUh|ryP M2nscVE2KG2rbh?= M2jOZ2lvcGmkaYTzJIZwem2jdHnvckBw\iCILXHjeIlvKHO2cnXzd{BncWKncoOgZY5lKHCqb4PwbI9zgWyjdHnvckBw\iCveX;zbY4hdGmpaISgZ4hicW5? MoizNVA3ODB2OU[=
Rat Vascular Smooth Muscle Cells MkjmSpVv[3Srb36gRZN{[Xl? M1\pXlExKM7:TR?= MlPhNkBp NFzUVFhKdmirYnn0d{Bidmerb4TlcpNqdiCLST3pcoR2[2WmIHj5dIVzfHKxcHj5 NEnkcoMyODZ2MkOxOy=>
PC3 MmTQSpVv[3Srb36gRZN{[Xl? M1P3bFI2KM7:TR?= NYDuc|RbOSCq NFjOTJVKdmS3Y3XzJI1wenCqb3zv[4lk[WxiY3jhcodmew>? NHjhVHUyODd{MES3NS=>
PC3 M3viOG1q\3KjdHnvckBCe3OjeR?= NFrLSWkzPSEQvF2= NFn5eXIyKGh? NXHNZZRGUW6qaXLpeJMhfGinIFLNSmIuS01iYX7kJJRp\SCHR1[td5RqdXWuYYTl[EBucWe{YYTpc44> M2nh[VExPzJyNEex
PC3 M4jEXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUn5eYZ3OjVizszN MlvUNVchcA>? MU\Ec4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To NGPvXVIyODd{MES3NS=>
LNCaP NGPLelRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\YVpJ7OjVizszN NULzfpJSOTdiaB?= MV\Ec4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To NHrXSlIyODd{MES3NS=>
Rat hepatic stellate cells Ml7mSpVv[3Srb36gRZN{[Xl? NHPx[HE{OCEQvF2= NID0TnU1QCCq M3:2dmRqdWmwaYPo[ZMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDFdoszNCCjbnSg[IVkemWjc3XzJI5mfyCGTlGgd5lvfGinc3nz NH\M[IkyODh2NU[2Ny=>
Pancreatic acinar cells NYW3[oJETnWwY4Tpc44hSXO|YYm= M3PjdFExyqEQvF2= NXrOfWM6PzBibXnu MoHuVI91\W62aXH0[ZMhS0ONLYP0bY12dGG2ZXSgdIFv[3KnYYTpZ{Bmdnq7bXWgd4VkemW2aX;u M4DDdFEzPzR3MEiw
C2C12 M4TsOWZ2dmO2aX;uJGF{e2G7 MX6xNOKh|ryP MoP3OkBp M1ezT3Bz\X[nboTzJJRp\SC|ZYLpcoUheGixc4Doc5J6dGG2aX;uJI9nKEmUUz2xJIlv\HWlZXSgZpkhcW6|dXzpckBidmRxb4KgWG5HNc7z MVWxOlI3PzF{NB?=
PC 12 MnPmSpVv[3Srb36gRZN{[Xl? NYnWeIhOOTEEoN88US=> M1rQRVI1KGh? NVu3N41wSXS2ZX71ZZRmeyClYYTlZ4hwdGGvaX7lJIJqd3O7boTo[ZNqew>? NEjLUZgyPjJzOUSyOC=>
Cynomolgus monkey embryonic stem cells NV7SPYlDS3m2b4TvfIlkKEG|c3H5 NVrabod6OjBiwsXN MkDBNlQhcA>? MnHQVJJwdW:2ZYOgZ5lGWyClZXzsJJN2en[rdnHs NX;BVY55OTh7NEC4OVU>
TSGH 8301 MmnvUYloemG2aX;uJGF{e2G7 NFzPNVAzOCEEtV2= M2HRRVEhcA>? MX\JcoNz\WG|ZYOgZ4VtdCCvaXfyZZRqd25? M3\ue|E6QDl4NEe1
Swiss3T3 NXLnW5E3S2:ub375MYZwem2rbnegRZN{[Xl? NHjkfXIyOCEEtV2= MkDENVMh\A>? M37QPGlv[3KnYYPld{Bxem:|dHH0[UBk\WyuIHPvcI9vgS2ob4LtbY5oKGGldHn2bZR6 MlHlNlE1PjR7MEK=
HT22 NEfvXWtEgXSxdH;4bYMhSXO|YYm= M4W4W|ExKML3TR?= Moj1NVMhcA>? MV\Qdo91\WO2czDh[4FqdnO2IHfseZRidWG2ZT3pcoR2[2WmIH7leZJwdmGuIHTlZZRp NWLaRpF[OjJ6MUC4N|U>
Salivary gland stem cells MWjGeY5kfGmxbjDBd5NigQ>? NG\DXJoyOCEEtV2= NHm4fWM4KGR? MUXS[YR2[2W|IGPHV2Mhe2WwZYPj[Y5k\Q>? MmOzNlU5ODR3NkC=

多くの細胞株試験データを見る場合、クリックしてください

体内試験 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]

お薦めの試験操作(参考用のみ)

動物試験:[1] [7]
+ 展開
  • 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)
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 64 mg/mL (199.83 mM) warming
Water 14 mg/mL (43.71 mM)
Ethanol Insoluble
体内 順序で溶剤を入れること:
saline
10mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 320.26
化学式

C14H21N3O.2HCl

CAS No. 129830-38-2
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

よくある質問(FAQ)

  • 問題1:

    Is there any data about the Amax (maximum attraction luminosity) and extinction coefficient of this compound?

  • 回答:

    The wavelength we used to test HPLC is 260nm while the extinction coefficient is unknown.

  • 問題2:

    Could this product be used in cell culture? Do you have any reference for this application?

  • 回答:

    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.

ROCK信号経路図

ROCK Inhibitors with Unique Features

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID