Y-27632 2HCl

Catalog No.S1049

Y-27632 2HCl Chemical Structure

Molecular Weight(MW): 320.26

Y-27632 2HCl is a selective ROCK1 (p160ROCK) inhibitor with Ki of 140 nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.

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Cited by 53 Publications

6 Customer Reviews

  • 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.

    At day 8, cells were replated onto Matrigel-coated Transwell membranes at 106 cells/cm2 in the presence or absence of 10 mM Y-27632. TEER was measured at day 10, 2 days after replating.

    Science, 2017, 3(11):e1701679. 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.

    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.

  • 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.

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

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Biological Activity

Description Y-27632 2HCl is a selective ROCK1 (p160ROCK) inhibitor with Ki of 140 nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.
Targets
ROCK1 (p160ROCK) [1]
(Cell-free assay)
ROCK2 [6]
(Cell-free assay)
140 nM(Ki) 300 nM(Ki)
In vitro

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 NVrmT5I2TnWwY4Tpc44hSXO|YYm= NX\BRVhPOTBizszN MXyyJIg> NYrUd5pRTE2VTx?= MX;Jcohq[mm2czD0bIUh[XO|ZX3icJkhd2ZibXnjdo91fWK3bHXzJIFv\CCrboTldo1m\GmjdHWg[olt[W2nboTzJJRwKG[xcn2g[Zh1\W6mZXSgdJJw[2W|c3Xz MX25OlQ4PjV2
N1E-115 MYTGeY5kfGmxbjDBd5NigQ>? M4fVdFExKM7:TR?= M4DOTVIhcA>? NUXP[VY5TE2VTx?= M1X3OGlvcGmkaYTzJJRp\SCjc4PlcYJtgSCxZjDtbYNzd3S3YoXs[ZMh[W6mIHnueIVzdWWmaXH0[UBncWyjbXXueJMhfG9iZn;ycUBmgHSnbnTl[EBxem:lZYPz[ZM> MkPVPVY1PzZ3NB?=
HeLa MlzGSpVv[3Srb36gRZN{[Xl? MWKxNEDPxE1? NHHqUII{OCCvaX6= NVe5cngxUW6qaXLpeJMhfGinIH\vdo1ifGmxbjDv[kB{fHKnc4Og[olj\XK|IHHu[EB1cGViYYPz[Y1jdHlib3[geolv[3WuaX6tZ49vfGGrbnnu[{Bnd2OjbDDh[Ihme2mxboO= MmnOPVY3QDB5Mh?=
CCL39 MmrXSpVv[3Srb36gRZN{[Xl? NG\CV4o{OCEQvF2= MVGzNEBucW5? M3XtdGNwdXCuZYTlcJkh[WKxbHnzbIV{KGGldHn2ZZRqd25ib3[gUoEuUCCneHPoZY5o\XJiTljFNUBjgSCrboTl[5JqdnN? MnzpPVY6OzN6Mh?=
Mesothelial cells from rat mesentery MnvtTY53[XOrdnWgRZN{[Xl? M{D2UlMxKM7:TR?= MX:yNEBp NHf6T3hDdG:la4OgbY53[XOrdnWgZYN1cX[rdIm= MofhPVk{ODh5Mh?=
NIH3T3 MlzrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XmdFExKM7:TR?= NH;SPFcyQCCm NFHCWHlFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp NHntSIkyODB{MUO4Oi=>
Dbl-d MmHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnJNVAh|ryP NYTMTVV[OThiZB?= M3K5SHN1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp NHL1bIsyODB{MUO4Oi=>
Dbl-e NGTXeZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUCxNEDPxE1? NWXpPXp5OThiZB?= NF7PXmdOd2SncnH0[Yx6KGmwaHnibZR{KGOnbHyg[5Jwf3Sq MojpNVAxOjF|OE[=
mNET1-d NULiXZNWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrINVAh|ryP MorGNVgh\A>? MnvlV5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg> M3ftXVExODJzM{i2
mNET1-e MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXexNEDPxE1? Mn:yNVgh\A>? M4q0b3N1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp MonLNVAxOjF|OE[=
Ras-2 NXrhUI8zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\YeFkyOCEQvF2= NGLIWVIyQCCm NHKzOnFUfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? M{PWTFExODJzM{i2
Ras-4 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LmWVExKM7:TR?= MnjkNVgh\A>? M{XGfnN1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp M{LNOFExODJzM{i2
Src-1 M2fWV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3K1bVExKM7:TR?= NEn4eFgyQCCm M4PNPWRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> M1\GSVExODJzM{i2
Src-4 NVHpNHVIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV:xNEDPxE1? NFLJS2YyQCCm MnrBSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> M1HZSVExODJzM{i2
NIH3T3 NEDxVpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUKxNEDPxE1? MmPXNVgh\A>? MUHEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To NUXLUoZyOTByMkGzPFY>
Src-1 M1vBOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV:xNEDPxE1? NFjad3EyQCCm MnPmSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> MV6xNFAzOTN6Nh?=
Src-2 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\zNnBNOTBizszN NH25fJYyQCCm NYDkdZRlTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? M2riRVExODJzM{i2
SW620 NEfxeYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXOxNEDPxE1? M2XqfVE5KGR? MX;Ec4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To NXyzWJl3OTByMkGzPFY>
HCT15 MnmxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHLNVAh|ryP NGf2OWEyQCCm NUjTSGtVTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? NIn5TFMyODB{MUO4Oi=>
HCT116 MlPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPYNVAh|ryP MUexPEBl NXrmPJc3W3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh? MVKxNFAzOTN6Nh?=
LS174T NX:0V5I{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW[xNEDPxE1? NXnnUZV3OThiZB?= NYToXYRbVW:mZYLheIVtgSCrbnjpZol1eyClZXzsJIdzd3e2aB?= M{Hoc|ExODJzM{i2
Neonatal rat ventricular myocytes MUjGeY5kfGmxbjDBd5NigQ>? NE\WR|kyOCEQvF2= MnqwOFghcA>? MYHJcohq[mm2czDFWE0yNWmwZIXj[YQhcW6lcnXhd4V{KGmwIIDyc5RmcW5ic4nueIhme2m|LDDj[YxtKHOrenWgZY5lKG27b3\pZpJqdGyjcjDvdodidmm8YYTpc44> MWexNFM5PjZzMx?=
Stellate Cell M3TXemZ2dmO2aX;uJGF{e2G7 NHewPGozPSEQvF2= NVLh[ItsOTVibXnu NEO5WG1KdmirYnn0d{Bnd3KvYYTpc44hd2ZiRj3hZ5RqdiC|dILld5Mh\mmkZYLzJIFv\CCyaH;zdIhwenmuYYTpc44hd2ZibYnvd4lvKGyrZ3j0JINp[Wmw NWTDVFB[OTB4MEC0PVY>
Rat Vascular Smooth Muscle Cells MWPGeY5kfGmxbjDBd5NigQ>? NX\1cWJnOTBizszN MkC5NkBp MofTTY5pcWKrdIOgZY5ocW:2ZX7zbY4hUUlvaX7keYNm\CCqeYDldpRzd3CqeR?= NHzqVZUyODZ2MkOxOy=>
PC3 NG\BZ4VHfW6ldHnvckBCe3OjeR?= NGPPTZczPSEQvF2= Mo[zNUBp NGfVfZpKdmS3Y3XzJI1wenCqb3zv[4lk[WxiY3jhcodmew>? MYGxNFczODR5MR?=
PC3 M1PSem1q\3KjdHnvckBCe3OjeR?= MYOyOUDPxE1? M17mc|EhcA>? MkXhTY5pcWKrdIOgeIhmKEKPRlKtR20h[W6mIITo[UBGT0Zvc4TpcZVt[XSnZDDtbYdz[XSrb36= MY[xNFczODR5MR?=
PC3 NVXpZVVbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkmyNlUh|ryP NG\rTHQyPyCq NYP5NGpnTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? NHTmTZIyODd{MES3NS=>
LNCaP NVz3NHhuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHjNlUh|ryP NXTKVYNHOTdiaB?= NGHrZZZFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp MmLaNVA4OjB2N{G=
Rat hepatic stellate cells MYnGeY5kfGmxbjDBd5NigQ>? NXTJXWVLOzBizszN MUe0PEBp MVHEbY1qdmm|aHXzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRYLrNkwh[W6mIHTlZ5Jm[XOnczDu[ZchTE6DIIP5cpRp\XOrcx?= M4PzSVExQDR3Nk[z
Pancreatic acinar cells MoH6SpVv[3Srb36gRZN{[Xl? M1nzOVExyqEQvF2= MVy3NEBucW5? NX7tW5hNWG:2ZX70bYF1\XNiQ1PLMZN1cW23bHH0[YQheGGwY4LlZZRq[yCnbor5cYUhe2WlcnX0bY9v M3fFXFEzPzR3MEiw
C2C12 MV\GeY5kfGmxbjDBd5NigQ>? NXrvZpBVOTEEoN88US=> NHnIdGE3KGh? NX3qNlUxWHKndnXueJMhfGinIIPldolv\SCyaH;zdIhwenmuYYTpc44hd2ZiSWLTMVEhcW6mdXPl[EBjgSCrboP1cIlvKGGwZD;vdkBVVkZvzsG= NVTkeWlbOTZ{NkexNlQ>
PC 12 MWTGeY5kfGmxbjDBd5NigQ>? NXPjRXViOTEEoN88US=> MWiyOEBp NYDENYRUSXS2ZX71ZZRmeyClYYTlZ4hwdGGvaX7lJIJqd3O7boTo[ZNqew>? NWPwTVlmOTZ{MUm0NlQ>
Cynomolgus monkey embryonic stem cells NHntXJpEgXSxdH;4bYMhSXO|YYm= NUHWUpI4OjBiwsXN MVqyOEBp M3rRWnBzd22xdHXzJIN6TVNiY3XscEB{fXK4aY\hcC=> NVjUVnJrOTh7NEC4OVU>
TSGH 8301 Ml72UYloemG2aX;uJGF{e2G7 NUjIenByOjBiwsXN NVjRPXpFOSCq NILHN2ZKdmO{ZXHz[ZMh[2WubDDtbYdz[XSrb36= Mn;jNVk5QTZ2N{W=
Swiss3T3 NVS1eFlCS2:ub375MYZwem2rbnegRZN{[Xl? MoSyNVAhyrWP MlnXNVMh\A>? Mmr0TY5kemWjc3XzJJBzd3O2YYTlJINmdGxiY3;sc456NW[xcn3pcoch[WO2aY\peJk> NHHoWnUzOTR4NEmwNi=>
HT22 MVrDfZRwfG:6aXOgRZN{[Xl? NIHifWwyOCEEtV2= MU[xN{Bp M1K1bnBzd3SnY4TzJIFo[Wmwc4Sg[4x2fGGvYYTlMYlv\HWlZXSgcoV2em:wYXyg[IVifGh? MorDNlI5OTB6M{W=
Salivary gland stem cells M1fQ[2Z2dmO2aX;uJGF{e2G7 MnPVNVAhyrWP NH\Qfmk4KGR? NIPVVXBT\WS3Y3XzJHNIW0Nic3Xu[ZNk\W6lZR?= MmrENlU5ODR3NkC=

... Click to View More Cell Line Experimental Data

In vivo 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]

Protocol

Animal Research:[1] [7]
+ Expand
  • Animal Models: Male Wistar rats with spontaneous or induced hypertension; Swiss albino mice with Ehrlich ascites carcinoma
  • Formulation: Dissolved in DMSO, and diluted in saline (Rat); 0.9% NaCl (Mice)
  • Dosages: 30 mg/kg/day (Rat); 0-10 mg/kg (mice)
  • Administration: Orally (Rat); i.p. (Mice)
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 64 mg/mL warmed (199.83 mM)
Water 14 mg/mL (43.71 mM)
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
saline
For best results, use promptly after mixing.
10mg/mL

* 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.

Chemical Information

Molecular Weight 320.26
Formula

C14H21N3O.2HCl

CAS No. 129830-38-2
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID