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 50 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.

    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.

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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 M{TGWmZ2dmO2aX;uJGF{e2G7 NGLp[GIyOCEQvF2= MXiyJIg> NHO3OodFVVOR Mli5TY5pcWKrdIOgeIhmKGG|c3XtZox6KG:oIH3pZ5JwfHWkdXzld{BidmRiaX70[ZJu\WSrYYTlJIZqdGGvZX70d{B1dyCob4LtJIV5fGWwZHXkJJBzd2Onc4Pldy=> NIW5T|g6PjR5NkW0
N1E-115 MoXhSpVv[3Srb36gRZN{[Xl? M3L3S|ExKM7:TR?= NGO1dIEzKGh? MWjEUXNQ MWXJcohq[mm2czD0bIUh[XO|ZX3icJkhd2ZibXnjdo91fWK3bHXzJIFv\CCrboTldo1m\GmjdHWg[olt[W2nboTzJJRwKG[xcn2g[Zh1\W6mZXSgdJJw[2W|c3Xz NEXyO|E6PjR5NkW0
HeLa M{O3VmZ2dmO2aX;uJGF{e2G7 NFrhZZEyOCEQvF2= M4e1TlMxKG2rbh?= M1nNRmlvcGmkaYTzJJRp\SCob4LtZZRqd25ib3[gd5Rz\XO|IH\pZoVzeyCjbnSgeIhmKGG|c3XtZox6KG:oII\pcoN2dGmwLXPvcpRicW6rbneg[o9k[WxiYXTo[ZNqd26| M{jIbFk3PjhyN{K=
CCL39 M3XsTmZ2dmO2aX;uJGF{e2G7 M{XjUFMxKM7:TR?= NH3mNIM{OCCvaX6= NGTVOFJEd22ybHX0[Yx6KGGkb3zpd4hmeyCjY4TpeoF1cW:wIH;mJG5iNUhiZYjjbIFv\2W{IF7ISVEh[nliaX70[YdzcW6| NYDPUHV7QTZ7M{O4Ni=>
Mesothelial cells from rat mesentery NFf6[GpKdn[jc3n2[UBCe3OjeR?= NWDoR4RlOzBizszN M4D1OlIxKGh? NVLmWVBiSmyxY3vzJIlvfmG|aY\lJIFkfGm4aYT5 MVi5PVMxQDd{
NIH3T3 M17aSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;vb|ExKM7:TR?= NHT3dmoyQCCm MnjuSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> NVq0WGk5OTByMkGzPFY>
Dbl-d M3vCPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MomzNVAh|ryP Mkn1NVgh\A>? NUG3fZd4W3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh? MmXrNVAxOjF|OE[=
Dbl-e Mkf2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonmNVAh|ryP NWfCfpJXOThiZB?= NYTCNZhJVW:mZYLheIVtgSCrbnjpZol1eyClZXzsJIdzd3e2aB?= NEnhRnoyODB{MUO4Oi=>
mNET1-d MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\pcphYOTBizszN NULlcHZIOThiZB?= M{XCOHN1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp NHP6VYkyODB{MUO4Oi=>
mNET1-e MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXHNVAh|ryP MmDLNVgh\A>? NWDNdJFwW3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh? NVnrTlVHOTByMkGzPFY>
Ras-2 NEPSbm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2T0blExKM7:TR?= Mnf6NVgh\A>? MVvTeJJwdmeueTDpcohq[mm2czDj[YxtKGe{b4f0bC=> NV[4Z|dqOTByMkGzPFY>
Ras-4 M{TTdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TUdVExKM7:TR?= MUSxPEBl M2HldnN1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp NUjxXoV3OTByMkGzPFY>
Src-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3H1TVExKM7:TR?= NYfJNZV6OThiZB?= M{T4UGRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> NI[xeWgyODB{MUO4Oi=>
Src-4 NGPJWYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXqxNEDPxE1? NWDQUYFjOThiZB?= MkLUSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> NXPiPYU1OTByMkGzPFY>
NIH3T3 NHr2WG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWKxNEDPxE1? MYCxPEBl NXvpRVV{TG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? NU\Hd3NGOTByMkGzPFY>
Src-1 NH[wOo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NES5cHAyOCEQvF2= M4TCR|E5KGR? MV;Ec4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To M4nLTFExODJzM{i2
Src-2 NXXjdFNwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUKxNEDPxE1? MXexPEBl NWfKVoQ1TG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? MWGxNFAzOTN6Nh?=
SW620 NGr6TYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXlOZdJOTBizszN NEK2eIQyQCCm MVrEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To MmjmNVAxOjF|OE[=
HCT15 NGPH[GZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzBW|gyOCEQvF2= M33LflE5KGR? MY\Ec4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To MX:xNFAzOTN6Nh?=
HCT116 M2\HZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUH0VWUzOTBizszN MnjHNVgh\A>? MYrTeJJwdmeueTDpcohq[mm2czDj[YxtKGe{b4f0bC=> NHLlPIgyODB{MUO4Oi=>
LS174T M1vWdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUWxNEDPxE1? MUGxPEBl MYjNc4RmemG2ZXz5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp MXixNFAzOTN6Nh?=
Neonatal rat ventricular myocytes NXPhbVdbTnWwY4Tpc44hSXO|YYm= M2P6b|ExKM7:TR?= NV7ve25oPDhiaB?= MoHLTY5pcWKrdIOgSXQuOS2rbnT1Z4VlKGmwY4LlZZNmeyCrbjDwdo91\WmwIIP5cpRp\XOrczygZ4VtdCC|aYrlJIFv\CCveX;mbYJzcWyuYYKgc5Jo[W6renH0bY9v MoP6NVA{QDZ4MUO=
Stellate Cell NH71RnJHfW6ldHnvckBCe3OjeR?= M1XW[VI2KM7:TR?= NXvy[5FOOTVibXnu Moj2TY5pcWKrdIOg[o9zdWG2aX;uJI9nKEZvYXP0bY4he3S{ZYPzJIZq[mW{czDhcoQheGixc4Doc5J6dGG2aX;uJI9nKG27b4PpckBtcWeqdDDjbIFqdg>? NWTmPYVFOTB4MEC0PVY>
Rat Vascular Smooth Muscle Cells MkjFSpVv[3Srb36gRZN{[Xl? NFSyNWQyOCEQvF2= NWi3WXpDOiCq M4HCbGlvcGmkaYTzJIFv\2mxdHXud4lvKEmLLXnu[JVk\WRiaInw[ZJ1em:yaIm= Mm\sNVA3PDJ|MUe=
PC3 NFK0U3NHfW6ldHnvckBCe3OjeR?= MVmyOUDPxE1? MkW5NUBp NHnKOI1KdmS3Y3XzJI1wenCqb3zv[4lk[WxiY3jhcodmew>? NUTVXm82OTB5MkC0O|E>
PC3 NInoXGJOcWe{YYTpc44hSXO|YYm= MYmyOUDPxE1? NHfVcngyKGh? Mn\3TY5pcWKrdIOgeIhmKEKPRlKtR20h[W6mIITo[UBGT0Zvc4TpcZVt[XSnZDDtbYdz[XSrb36= NUXEN5YyOTB5MkC0O|E>
PC3 NFLZVFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHWNlUh|ryP NFnTO|UyPyCq M4fGNmRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> NHLFU3QyODd{MES3NS=>
LNCaP M4KyZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFP5dJMzPSEQvF2= M{DSZVE4KGh? MXnEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To NEK3OVAyODd{MES3NS=>
Rat hepatic stellate cells NHzCcXFHfW6ldHnvckBCe3OjeR?= M{faVFMxKM7:TR?= MXS0PEBp NVfM[JhTTGmvaX7pd4hmeyC2aHWgdIhwe3Cqb4L5cIF1cW:wIH;mJGVzczJuIHHu[EBl\WO{ZXHz[ZMhdmW5IFTORUB{gW62aHXzbZM> NIXPZnQyODh2NU[2Ny=>
Pancreatic acinar cells Mli5SpVv[3Srb36gRZN{[Xl? NIHYcJoyOMLizszN NEiw[XI4OCCvaX6= M3;SS3BwfGWwdHnheIV{KEOFSz3zeIlufWyjdHXkJJBidmO{ZXH0bYMh\W68eX3lJJNm[3KndHnvci=> Ml7RNVI4PDVyOEC=
C2C12 NWH1TmdWTnWwY4Tpc44hSXO|YYm= NG\2VHMyOMLizszN M4XxXlYhcA>? MV7QdoV3\W62czD0bIUhe2W{aX7lJJBpd3OyaH;yfYxifGmxbjDv[kBKWlNvMTDpcoR2[2WmIHL5JIlve3WuaX6gZY5lN2:{IGTOSk3PuQ>? MoWwNVYzPjdzMkS=
PC 12 NI\4NVNHfW6ldHnvckBCe3OjeR?= NWTVcWpoOTEEoN88US=> NVXoeZhqOjRiaB?= M4POPGF1fGWwdXH0[ZMh[2G2ZXPoc4xidWmwZTDibY9{gW62aHXzbZM> M1nBO|E3OjF7NEK0
Cynomolgus monkey embryonic stem cells MkCxR5l1d3SxeHnjJGF{e2G7 NYrMT2dCOjBiwsXN M2LmZVI1KGh? NH7lbYRRem:vb4Tld{BkgUWVIHPlcIwhe3W{dnn2ZYw> NVz4RWV{OTh7NEC4OVU>
TSGH 8301 NEns[|dOcWe{YYTpc44hSXO|YYm= NFTEVZMzOCEEtV2= NUTheFNuOSCq NH3VOmpKdmO{ZXHz[ZMh[2WubDDtbYdz[XSrb36= NEW3bZIyQTh7NkS3OS=>
Swiss3T3 M33vN2NwdG:weT3mc5JucW6pIFHzd4F6 NGjKT4QyOCEEtV2= M1O1UlE{KGR? MWnJcoNz\WG|ZYOgdJJwe3SjdHWgZ4VtdCClb3zvcpku\m:{bXnu[{Bi[3Srdnn0fS=> M2TZUlIyPDZ2OUCy
HT22 M2T2NGN6fG:2b4jpZ{BCe3OjeR?= M2ezdVExKML3TR?= NGTpNXAyOyCq MYDQdo91\WO2czDh[4FqdnO2IHfseZRidWG2ZT3pcoR2[2WmIH7leZJwdmGuIHTlZZRp NXT3WZJyOjJ6MUC4N|U>
Salivary gland stem cells M1HRT2Z2dmO2aX;uJGF{e2G7 NYLh[ZNJOTBiwsXN NXfpNodjPyCm M3HPdXJm\HWlZYOgV2dUSyC|ZX7ld4NmdmOn NVuwTZVEOjV6MES1OlA>

... 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

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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