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 25896.00
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文献中の使用例(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 M{naUWZ2dmO2aX;uJGF{e2G7 NGXxWYsyOCEQvF2= MWqyJIg> M3n5SWROW09? M2HrNmlvcGmkaYTzJJRp\SCjc4PlcYJtgSCxZjDtbYNzd3S3YoXs[ZMh[W6mIHnueIVzdWWmaXH0[UBncWyjbXXueJMhfG9iZn;ycUBmgHSnbnTl[EBxem:lZYPz[ZM> NWLOXFN5QTZ2N{[1OC=>
N1E-115 NH\BZpFHfW6ldHnvckBCe3OjeR?= MnLyNVAh|ryP M2PIUFIhcA>? NIK4UFJFVVOR NFv5eFFKdmirYnn0d{B1cGViYYPz[Y1jdHlib3[gcYlkem:2dXL1cIV{KGGwZDDpcpRmem2nZHnheIUh\mmuYX3lcpR{KHSxIH\vdo0h\Xi2ZX7k[YQheHKxY3Xzd4V{ M{C2VFk3PDd4NUS=
HeLa NUSxOlM6TnWwY4Tpc44hSXO|YYm= MYqxNEDPxE1? MkL3N|AhdWmw M2m1NWlvcGmkaYTzJJRp\SCob4LtZZRqd25ib3[gd5Rz\XO|IH\pZoVzeyCjbnSgeIhmKGG|c3XtZox6KG:oII\pcoN2dGmwLXPvcpRicW6rbneg[o9k[WxiYXTo[ZNqd26| M4nuU|k3PjhyN{K=
CCL39 MYrGeY5kfGmxbjDBd5NigQ>? M3S1fFMxKM7:TR?= Mm\GN|AhdWmw NFLZbWpEd22ybHX0[Yx6KGGkb3zpd4hmeyCjY4TpeoF1cW:wIH;mJG5iNUhiZYjjbIFv\2W{IF7ISVEh[nliaX70[YdzcW6| MVK5Olk{Ozh{
Mesothelial cells from rat mesentery M{njSGlvfmG|aY\lJGF{e2G7 M2XubFMxKM7:TR?= M{DyOVIxKGh? NX6wb5RtSmyxY3vzJIlvfmG|aY\lJIFkfGm4aYT5 NEDEcZI6QTNyOEey
NIH3T3 M{TRc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3qXVcyOCEQvF2= NInXcYUyQCCm M{fBVGRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> NWq3cFVHOTByMkGzPFY>
Dbl-d NGLMU2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXINVAh|ryP NYH1e5NNOThiZB?= Mlq2V5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NUjkNWhQOTByMkGzPFY>
Dbl-e NHTYSmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnmTGE3OTBizszN M2\rW|E5KGR? MXTNc4RmemG2ZXz5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp MUmxNFAzOTN6Nh?=
mNET1-d NGTTTIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWKxNEDPxE1? MlHDNVgh\A>? MUPTeJJwdmeueTDpcohq[mm2czDj[YxtKGe{b4f0bC=> NVjWcnJZOTByMkGzPFY>
mNET1-e NGO0PZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrBNVAh|ryP NXrlPJJLOThiZB?= NYPaRoZ{W3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh? M2fEcVExODJzM{i2
Ras-2 MnHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3OU41GOTBizszN MkL4NVgh\A>? NXXiTVlFW3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh? MYWxNFAzOTN6Nh?=
Ras-4 MlywS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjXNVAh|ryP MVSxPEBl M3z5dXN1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp NF30TW8yODB{MUO4Oi=>
Src-1 NWrzcIQ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nMTFExKM7:TR?= NHjubWsyQCCm MVLEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To M3H1blExODJzM{i2
Src-4 MlnOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXDeHFROTBizszN NWHpcJVpOThiZB?= MoHDSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> NUDw[IhVOTByMkGzPFY>
NIH3T3 NWq4[mFHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLJNVlmOTBizszN M1r4RlE5KGR? MkHBSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> NILvfnIyODB{MUO4Oi=>
Src-1 MmHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVf6XWVoOTBizszN M{\3WFE5KGR? M3X0OmRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> MnfXNVAxOjF|OE[=
Src-2 M1nK[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDMNVAh|ryP MY[xPEBl NGTlSlhFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp NWHkfWNoOTByMkGzPFY>
SW620 MmfzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVz2U3pNOTBizszN NIXocnEyQCCm MYHEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To MlnkNVAxOjF|OE[=
HCT15 NI[zeGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn6xNVAh|ryP M4\JbVE5KGR? MV\Ec4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To MVmxNFAzOTN6Nh?=
HCT116 M3jN[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU[xNEDPxE1? NEP5O4oyQCCm M3ixWXN1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp Moe2NVAxOjF|OE[=
LS174T M1;rc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1:0elExKM7:TR?= M1;adVE5KGR? NEKye3ROd2SncnH0[Yx6KGmwaHnibZR{KGOnbHyg[5Jwf3Sq MorJNVAxOjF|OE[=
Neonatal rat ventricular myocytes NH7URVlHfW6ldHnvckBCe3OjeR?= MYmxNEDPxE1? M1O0TFQ5KGh? MmHCTY5pcWKrdIOgSXQuOS2rbnT1Z4VlKGmwY4LlZZNmeyCrbjDwdo91\WmwIIP5cpRp\XOrczygZ4VtdCC|aYrlJIFv\CCveX;mbYJzcWyuYYKgc5Jo[W6renH0bY9v MljBNVA{QDZ4MUO=
Stellate Cell MWrGeY5kfGmxbjDBd5NigQ>? MoX0NlUh|ryP M4rKNFE2KG2rbh?= MV7Jcohq[mm2czDmc5Ju[XSrb36gc4YhTi2jY4TpckB{fHKnc4Og[olj\XK|IHHu[EBxcG:|cHjvdplt[XSrb36gc4YhdXmxc3nuJIxq\2i2IHPoZYlv NFXKcVQyODZyMES5Oi=>
Rat Vascular Smooth Muscle Cells Mo\iSpVv[3Srb36gRZN{[Xl? MoLZNVAh|ryP NYG5b4tlOiCq NITpUIVKdmirYnn0d{Bidmerb4TlcpNqdiCLST3pcoR2[2WmIHj5dIVzfHKxcHj5 NHHCfm8yODZ2MkOxOy=>
PC3 NUTleIRvTnWwY4Tpc44hSXO|YYm= NXTxcGZ[OjVizszN MlHhNUBp M3XUPGlv\HWlZYOgcY9zeGixbH;nbYNidCClaHHu[4V{ NGe3fXQyODd{MES3NS=>
PC3 Mk\CUYloemG2aX;uJGF{e2G7 NFLDUY0zPSEQvF2= MkXBNUBp M2\ocGlvcGmkaYTzJJRp\SCETV\CMWNOKGGwZDD0bIUhTUeILYP0bY12dGG2ZXSgcYloemG2aX;u M2PkOlExPzJyNEex
PC3 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITl[5UzPSEQvF2= MUGxO{Bp NHvsd|ZFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp MYOxNFczODR5MR?=
LNCaP MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mly0NlUh|ryP NXzKWHVwOTdiaB?= NH7Ye3lFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp NUK3U|RiOTB5MkC0O|E>
Rat hepatic stellate cells NHj1RmVHfW6ldHnvckBCe3OjeR?= MonmN|Ah|ryP MlTvOFghcA>? NVHtUnpwTGmvaX7pd4hmeyC2aHWgdIhwe3Cqb4L5cIF1cW:wIH;mJGVzczJuIHHu[EBl\WO{ZXHz[ZMhdmW5IFTORUB{gW62aHXzbZM> NF\QXYoyODh2NU[2Ny=>
Pancreatic acinar cells MYnGeY5kfGmxbjDBd5NigQ>? NVrqfnFYOTEEoN88US=> Moj2O|AhdWmw MX\Qc5RmdnSrYYTld{BES0tvc4TpcZVt[XSnZDDwZY5kemWjdHnjJIVvgnmvZTDz[YNz\XSrb36= M3TKXlEzPzR3MEiw
C2C12 M3;QU2Z2dmO2aX;uJGF{e2G7 MnHCNVDDqM7:TR?= MXG2JIg> NIrYdXBRemW4ZX70d{B1cGVic3XybY5mKHCqb4PwbI9zgWyjdHnvckBw\iCLUmOtNUBqdmS3Y3XkJIJ6KGmwc4XsbY4h[W6mL3;yJHRPTi4QsR?= NEHWUnYyPjJ4N{GyOC=>
PC 12 MXrGeY5kfGmxbjDBd5NigQ>? M3eyc|ExyqEQvF2= NX;2cJNxOjRiaB?= NVm0XZlMSXS2ZX71ZZRmeyClYYTlZ4hwdGGvaX7lJIJqd3O7boTo[ZNqew>? MV:xOlIyQTR{NB?=
Cynomolgus monkey embryonic stem cells MXfDfZRwfG:6aXOgRZN{[Xl? MlvHNlAhyrWP NUTGXlYzOjRiaB?= NX7qPXZxWHKxbX;0[ZMh[3mHUzDj[YxtKHO3co\peoFt MXSxPFk1ODh3NR?=
TSGH 8301 Ml3kUYloemG2aX;uJGF{e2G7 MX6yNEDDvU1? NVriWHB7OSCq NF\UNlNKdmO{ZXHz[ZMh[2WubDDtbYdz[XSrb36= NIWycJIyQTh7NkS3OS=>
Swiss3T3 NYW0cFlLS2:ub375MYZwem2rbnegRZN{[Xl? MmH0NVAhyrWP MkW4NVMh\A>? MnHaTY5kemWjc3XzJJBzd3O2YYTlJINmdGxiY3;sc456NW[xcn3pcoch[WO2aY\peJk> MkXDNlE1PjR7MEK=
HT22 MVrDfZRwfG:6aXOgRZN{[Xl? NY\ZZWpbOTBiwsXN MVSxN{Bp NYnUcJJoWHKxdHXjeJMh[WejaX7zeEBodHW2YX3heIUucW6mdXPl[EBv\XW{b37hcEBl\WG2aB?= Mo\JNlI5OTB6M{W=
Salivary gland stem cells NF25dnFHfW6ldHnvckBCe3OjeR?= M2PTbFExKML3TR?= NFn6Nlg4KGR? Ml3KVoVlfWOnczDTS3NEKHOnbnXzZ4Vv[2V? MlfhNlU5ODR3NkC=

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
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.

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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