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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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。
靶点
ROCK1 (p160ROCK) [1]
(Cell-free assay)
ROCK2 [6]
(Cell-free assay)
140 nM(Ki) 300 nM(Ki)
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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Swiss 3T3 cells M3rmfmZ2dmO2aX;uJGF{e2G7 M{T1b|ExKM7:TR?= NE[yPW4zKGh? Mk\1SG1UVw>? MknCTY5pcWKrdIOgeIhmKGG|c3XtZox6KG:oIH3pZ5JwfHWkdXzld{BidmRiaX70[ZJu\WSrYYTlJIZqdGGvZX70d{B1dyCob4LtJIV5fGWwZHXkJJBzd2Onc4Pldy=> MmDMPVY1PzZ3NB?=
N1E-115 NX7SWplpTnWwY4Tpc44hSXO|YYm= NVLwdmRXOTBizszN Mo\sNkBp M3nmeGROW09? M2TLUWlvcGmkaYTzJJRp\SCjc4PlcYJtgSCxZjDtbYNzd3S3YoXs[ZMh[W6mIHnueIVzdWWmaXH0[UBncWyjbXXueJMhfG9iZn;ycUBmgHSnbnTl[EBxem:lZYPz[ZM> NEWydGQ6PjR5NkW0
HeLa MUXGeY5kfGmxbjDBd5NigQ>? NIe1engyOCEQvF2= MmHuN|AhdWmw MXHJcohq[mm2czD0bIUh\m:{bXH0bY9vKG:oIIP0doV{eyCoaXLldpMh[W6mIITo[UBie3OnbXLsfUBw\iC4aX7jeYxqdi2lb370ZYlvcW6pIH\vZ4FtKGGmaHXzbY9vew>? NXTpdXhUQTZ4OEC3Ni=>
CCL39 M2HadWZ2dmO2aX;uJGF{e2G7 NWjYNVdoOzBizszN NFr0Nnk{OCCvaX6= MWPDc41xdGW2ZXz5JIFjd2yrc3jld{Bi[3SrdnH0bY9vKG:oIF7hMWgh\XilaHHu[4VzKE6KRUGgZpkhcW62ZXfybY5{ M2WySlk3QTN|OEK=
Mesothelial cells from rat mesentery NWHhRlJWUW64YYPpeoUhSXO|YYm= NHPmUoc{OCEQvF2= NYHhVIxOOjBiaB?= NHX1UldDdG:la4OgbY53[XOrdnWgZYN1cX[rdIm= Mn;VPVk{ODh5Mh?=
NIH3T3 NEHZcFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmP1NVAh|ryP NHf5bHYyQCCm NUXV[4pPTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? MnT0NVAxOjF|OE[=
Dbl-d NWLpUFNqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPGdFkyOCEQvF2= M3jrUVE5KGR? MkXKV5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg> M{jiWFExODJzM{i2
Dbl-e M1;tOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLlVZN2OTBizszN NET2PXkyQCCm NYWzdnJnVW:mZYLheIVtgSCrbnjpZol1eyClZXzsJIdzd3e2aB?= NXLlOmtVOTByMkGzPFY>
mNET1-d NFX0SopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3TVIQ6OTBizszN MXmxPEBl NH7Yd|FUfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MmGwNVAxOjF|OE[=
mNET1-e M4LRWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXqxNEDPxE1? NEWwZ3gyQCCm NXezR3VsW3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh? NXG3[456OTByMkGzPFY>
Ras-2 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzFe4djOTBizszN NIrVPWUyQCCm NILLWoZUfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NVXtbXNwOTByMkGzPFY>
Ras-4 MnGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVKxNEDPxE1? MUmxPEBl NIjZZXRUfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NXr4UmVLOTByMkGzPFY>
Src-1 NH\qfZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWqy[lE5OTBizszN MnOzNVgh\A>? NWjnPXB[TG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? NVfWPIdkOTByMkGzPFY>
Src-4 NH\YVXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWWxNEDPxE1? MnnFNVgh\A>? NVj6[2RSTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? M{fSN|ExODJzM{i2
NIH3T3 M{TYdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrhOpZPOTBizszN M3\ieVE5KGR? MnHlSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> M1z4XlExODJzM{i2
Src-1 NVTGWIM5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7zSW4yOCEQvF2= NFvVNI4yQCCm MofQSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> MXyxNFAzOTN6Nh?=
Src-2 NV\CSFFzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXOxNEDPxE1? MUWxPEBl MXrEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To M4O0cVExODJzM{i2
SW620 NIe0OHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYCxNEDPxE1? MYmxPEBl MVzEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To M{juNlExODJzM{i2
HCT15 MmXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPqTGsyOCEQvF2= MUKxPEBl M{HpT2Rw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> MnvuNVAxOjF|OE[=
HCT116 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmG0NVAh|ryP MlzFNVgh\A>? MnrOV5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NEXZXm4yODB{MUO4Oi=>
LS174T NInrXZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHtbllHOTBizszN M1T0SlE5KGR? NIHGW29Od2SncnH0[Yx6KGmwaHnibZR{KGOnbHyg[5Jwf3Sq M2W3c|ExODJzM{i2
Neonatal rat ventricular myocytes NULyNYZMTnWwY4Tpc44hSXO|YYm= M1W1WFExKM7:TR?= MXW0PEBp MY\Jcohq[mm2czDFWE0yNWmwZIXj[YQhcW6lcnXhd4V{KGmwIIDyc5RmcW5ic4nueIhme2m|LDDj[YxtKHOrenWgZY5lKG27b3\pZpJqdGyjcjDvdodidmm8YYTpc44> NHrqZosyODN6Nk[xNy=>
Stellate Cell NE\KXHlHfW6ldHnvckBCe3OjeR?= NHjUOIMzPSEQvF2= NEe5c2QyPSCvaX6= MYnJcohq[mm2czDmc5Ju[XSrb36gc4YhTi2jY4TpckB{fHKnc4Og[olj\XK|IHHu[EBxcG:|cHjvdplt[XSrb36gc4YhdXmxc3nuJIxq\2i2IHPoZYlv NH:3TGkyODZyMES5Oi=>
Rat Vascular Smooth Muscle Cells MmDjSpVv[3Srb36gRZN{[Xl? M4PXWFExKM7:TR?= NHHidIUzKGh? MWXJcohq[mm2czDhcodqd3SnboPpckBKUS2rbnT1Z4VlKGi7cHXyeJJweGi7 NXW3XIVbOTB4NEKzNVc>
PC3 NYLONIROTnWwY4Tpc44hSXO|YYm= MorsNlUh|ryP NHK2UVEyKGh? MVrJcoR2[2W|IH3vdpBpd2yxZ3njZYwh[2ijbnfldy=> MkTzNVA4OjB2N{G=
PC3 MlnsUYloemG2aX;uJGF{e2G7 NVfqNGd4OjVizszN M2T1b|EhcA>? M3:wcWlvcGmkaYTzJJRp\SCETV\CMWNOKGGwZDD0bIUhTUeILYP0bY12dGG2ZXSgcYloemG2aX;u MlW4NVA4OjB2N{G=
PC3 MlLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjLdnRTOjVizszN Mn:0NVchcA>? M4jFTWRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> M{jrTVExPzJyNEex
LNCaP NH72cGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX[yOUDPxE1? NGntRYMyPyCq M3[zc2Rw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> NV\U[I51OTB5MkC0O|E>
Rat hepatic stellate cells MmTpSpVv[3Srb36gRZN{[Xl? MkeyN|Ah|ryP NFy5fJk1QCCq NGHEbpNFcW2rbnnzbIV{KHSqZTDwbI9{eGixconsZZRqd25ib3[gSZJsOixiYX7kJIRm[3KnYYPld{Bv\XdiRF7BJJN6dnSqZYPpdy=> M{\yV|ExQDR3Nk[z
Pancreatic acinar cells M3\pPWZ2dmO2aX;uJGF{e2G7 MkO4NVDDqM7:TR?= NVX3OGtzPzBibXnu NVrpc5ZXWG:2ZX70bYF1\XNiQ1PLMZN1cW23bHH0[YQheGGwY4LlZZRq[yCnbor5cYUhe2WlcnX0bY9v NXTOUFhqOTJ5NEWwPFA>
C2C12 M1zpTmZ2dmO2aX;uJGF{e2G7 NV7ZXYY5OTEEoN88US=> NFXWdm03KGh? NWrm[nVkWHKndnXueJMhfGinIIPldolv\SCyaH;zdIhwenmuYYTpc44hd2ZiSWLTMVEhcW6mdXPl[EBjgSCrboP1cIlvKGGwZD;vdkBVVkZvzsG= M2TZelE3OjZ5MUK0
PC 12 M{CzdmZ2dmO2aX;uJGF{e2G7 MYWxNOKh|ryP MWmyOEBp MoDhRZR1\W63YYTld{Bk[XSnY3jvcIFucW6nIHLpc5N6dnSqZYPpdy=> NWfsXoZEOTZ{MUm0NlQ>
Cynomolgus monkey embryonic stem cells M{m0TWN6fG:2b4jpZ{BCe3OjeR?= MV:yNEDDvU1? Ml\hNlQhcA>? Mlf5VJJwdW:2ZYOgZ5lGWyClZXzsJJN2en[rdnHs MmPkNVg6PDB6NUW=
TSGH 8301 Mn;rUYloemG2aX;uJGF{e2G7 NWe5RmVOOjBiwsXN M1OwOlEhcA>? M{fEN2lv[3KnYYPld{Bk\WyuIH3p[5JifGmxbh?= Mn7WNVk5QTZ2N{W=
Swiss3T3 MVvDc4xwdnlvZn;ycYlv\yCDc4PhfS=> MXGxNEDDvU1? NED1cWoyOyCm MmXYTY5kemWjc3XzJJBzd3O2YYTlJINmdGxiY3;sc456NW[xcn3pcoch[WO2aY\peJk> MX[yNVQ3PDlyMh?=
HT22 NI[1d4tEgXSxdH;4bYMhSXO|YYm= M{\tT|ExKML3TR?= MXWxN{Bp MXvQdo91\WO2czDh[4FqdnO2IHfseZRidWG2ZT3pcoR2[2WmIH7leZJwdmGuIHTlZZRp MkXhNlI5OTB6M{W=
Salivary gland stem cells NGHyVWVHfW6ldHnvckBCe3OjeR?= NUD0[lU3OTBiwsXN MlnOO{Bl NXT3NIw{WmWmdXPld{BUT1OFIIPlcoV{[2WwY3W= NWS1TYxJOjV6MES1OlA>

... 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]

プロトコル(参考用のみ)

動物実験:[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 <1 mg/mL
体内 saline 10mg/mL

* <1 mg/mlは製品が微弱に溶解する或いは溶解しないことを示します。
* 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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID