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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In DMSO USD 156 In stock
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Cited by 48 Publications

5 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.

    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.

Purity & Quality Control

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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 MUDGeY5kfGmxbjDBd5NigQ>? M3fqRlExKM7:TR?= MWmyJIg> NYHIbolWTE2VTx?= NUf5OJFyUW6qaXLpeJMhfGinIHHzd4Vu[my7IH;mJI1q[3KxdIXieYxmeyCjbnSgbY51\XKvZXTpZZRmKG[rbHHt[Y51eyC2bzDmc5JuKGW6dHXu[IVlKHC{b3Pld5Nmew>? NXfVbW1oQTZ2N{[1OC=>
N1E-115 MUTGeY5kfGmxbjDBd5NigQ>? NIr3fmYyOCEQvF2= NVHpUIR7OiCq MVzEUXNQ NUDEVpdxUW6qaXLpeJMhfGinIHHzd4Vu[my7IH;mJI1q[3KxdIXieYxmeyCjbnSgbY51\XKvZXTpZZRmKG[rbHHt[Y51eyC2bzDmc5JuKGW6dHXu[IVlKHC{b3Pld5Nmew>? MlP4PVY1PzZ3NB?=
HeLa NHi3bnhHfW6ldHnvckBCe3OjeR?= NIHBTJUyOCEQvF2= NV\qSW11OzBibXnu Mo\ZTY5pcWKrdIOgeIhmKG[xcn3heIlwdiCxZjDzeJJme3NiZnni[ZJ{KGGwZDD0bIUh[XO|ZX3icJkhd2ZidnnuZ5VtcW5vY3;ueIFqdmmwZzDmc4NidCCjZHjld4lwdnN? M1\VTlk3PjhyN{K=
CCL39 Mnr4SpVv[3Srb36gRZN{[Xl? NHj2VJo{OCEQvF2= M4fxR|MxKG2rbh?= NWfDOGt4S2:vcHzleIVtgSCjYn;sbZNp\XNiYXP0bZZifGmxbjDv[kBP[S2KIHX4Z4hidmencjDOTGUyKGK7IHnueIVoemmwcx?= NXTH[FV[QTZ7M{O4Ni=>
Mesothelial cells from rat mesentery NX\2R4FvUW64YYPpeoUhSXO|YYm= NYK5foU3OzBizszN MYSyNEBp MojERoxw[2u|IHnueoF{cX[nIHHjeIl3cXS7 MW[5PVMxQDd{
NIH3T3 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rTWlExKM7:TR?= MV[xPEBl NI[3TIlFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp MkPNNVAxOjF|OE[=
Dbl-d MlvHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVmxNEDPxE1? MkH1NVgh\A>? MlfQV5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NYLPWIZsOTByMkGzPFY>
Dbl-e MnrnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXONVAh|ryP MVWxPEBl NV;3ZmYxVW:mZYLheIVtgSCrbnjpZol1eyClZXzsJIdzd3e2aB?= M{\IVlExODJzM{i2
mNET1-d MnjwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkP0NVAh|ryP MkPXNVgh\A>? NF3wWVJUfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NWSwR5doOTByMkGzPFY>
mNET1-e MnnES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYixNEDPxE1? M1;GflE5KGR? NH;FXoFUfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MXqxNFAzOTN6Nh?=
Ras-2 NYjSZ4RPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPFTVIyOCEQvF2= MlP1NVgh\A>? NXnmRXByW3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh? NEDtNWUyODB{MUO4Oi=>
Ras-4 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MluxNVAh|ryP NWnZOHlpOThiZB?= MkjqV5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MmTWNVAxOjF|OE[=
Src-1 NHP1cnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILLZ4cyOCEQvF2= NHjRWHoyQCCm NVf1NFM3TG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? NVLueZF1OTByMkGzPFY>
Src-4 MmfDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoO2NVAh|ryP NID0RpUyQCCm NIPtNmNFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp NETZUWYyODB{MUO4Oi=>
NIH3T3 M1;QNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWKxNEDPxE1? NETzb5AyQCCm NY\6RnJoTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? NYrsSmplOTByMkGzPFY>
Src-1 NWTrdWh5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrCbGQ5OTBizszN MmjWNVgh\A>? M1zhXWRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> NUHEV2NKOTByMkGzPFY>
Src-2 NXzEVVVUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLjNVAh|ryP NUiyd3cxOThiZB?= MWPEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To NX;jfGJnOTByMkGzPFY>
SW620 NVjyS3c4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXWxNEDPxE1? MnLHNVgh\A>? MnntSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> MkLMNVAxOjF|OE[=
HCT15 MmfGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfvflAyOTBizszN MYKxPEBl NEDuZ4ZFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp NHT0OXYyODB{MUO4Oi=>
HCT116 MnnkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rLVVExKM7:TR?= MlK4NVgh\A>? NH3JPVJUfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NXTyS|d6OTByMkGzPFY>
LS174T NHnFbnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX[xNEDPxE1? NUjycGdSOThiZB?= NWXvfGZSVW:mZYLheIVtgSCrbnjpZol1eyClZXzsJIdzd3e2aB?= M4T1[FExODJzM{i2
Neonatal rat ventricular myocytes NXHjS2FyTnWwY4Tpc44hSXO|YYm= NIrTdlIyOCEQvF2= Mor1OFghcA>? MVjJcohq[mm2czDFWE0yNWmwZIXj[YQhcW6lcnXhd4V{KGmwIIDyc5RmcW5ic4nueIhme2m|LDDj[YxtKHOrenWgZY5lKG27b3\pZpJqdGyjcjDvdodidmm8YYTpc44> NUT0WVFTOTB|OE[2NVM>
Stellate Cell MUnGeY5kfGmxbjDBd5NigQ>? M1\3elI2KM7:TR?= Ml34NVUhdWmw MXPJcohq[mm2czDmc5Ju[XSrb36gc4YhTi2jY4TpckB{fHKnc4Og[olj\XK|IHHu[EBxcG:|cHjvdplt[XSrb36gc4YhdXmxc3nuJIxq\2i2IHPoZYlv MXqxNFYxODR7Nh?=
Rat Vascular Smooth Muscle Cells M2PufGZ2dmO2aX;uJGF{e2G7 NFK0RlIyOCEQvF2= M3KwblIhcA>? Mk\yTY5pcWKrdIOgZY5ocW:2ZX7zbY4hUUlvaX7keYNm\CCqeYDldpRzd3CqeR?= NV7Hbo92OTB4NEKzNVc>
PC3 NUPr[llsTnWwY4Tpc44hSXO|YYm= NEm1WGIzPSEQvF2= MWixJIg> MlWyTY5lfWOnczDtc5JxcG:ub3fpZ4FtKGOqYX7n[ZM> M3zV[|ExPzJyNEex
PC3 NHXoVGpOcWe{YYTpc44hSXO|YYm= NVvObJQ5OjVizszN MV:xJIg> NXLSdJNyUW6qaXLpeJMhfGinIFLNSmIuS01iYX7kJJRp\SCHR1[td5RqdXWuYYTl[EBucWe{YYTpc44> M{faSlExPzJyNEex
PC3 NEnjXlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPQOotGOjVizszN M1r1SlE4KGh? MWnEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To M2rKSlExPzJyNEex
LNCaP M1vmZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rUb|I2KM7:TR?= MlTWNVchcA>? NGTlWoFFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp MWGxNFczODR5MR?=
Rat hepatic stellate cells M4nJR2Z2dmO2aX;uJGF{e2G7 MUCzNEDPxE1? M3nOXFQ5KGh? M4e0OmRqdWmwaYPo[ZMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDFdoszNCCjbnSg[IVkemWjc3XzJI5mfyCGTlGgd5lvfGinc3nz M1Pm[|ExQDR3Nk[z
Pancreatic acinar cells NVP6THJ1TnWwY4Tpc44hSXO|YYm= NWjyXGd[OTEEoN88US=> NVnldIJqPzBibXnu NF;Ee5dRd3SnboTpZZRmeyCFQ1utd5RqdXWuYYTl[EBx[W6lcnXheIlkKGWweont[UB{\WO{ZYTpc44> NEL5bmcyOjd2NUC4NC=>
C2C12 MlzNSpVv[3Srb36gRZN{[Xl? M2TnSFExyqEQvF2= MX62JIg> MWrQdoV3\W62czD0bIUhe2W{aX7lJJBpd3OyaH;yfYxifGmxbjDv[kBKWlNvMTDpcoR2[2WmIHL5JIlve3WuaX6gZY5lN2:{IGTOSk3PuQ>? MnfGNVYzPjdzMkS=
PC 12 NWf5b|R[TnWwY4Tpc44hSXO|YYm= MlzONVDDqM7:TR?= NWLjZnc{OjRiaB?= MnS1RZR1\W63YYTld{Bk[XSnY3jvcIFucW6nIHLpc5N6dnSqZYPpdy=> NYjlN2lXOTZ{MUm0NlQ>
Cynomolgus monkey embryonic stem cells NIPIeFZEgXSxdH;4bYMhSXO|YYm= MYKyNEDDvU1? Ml;ZNlQhcA>? M2OzUHBzd22xdHXzJIN6TVNiY3XscEB{fXK4aY\hcC=> M1nWZVE5QTRyOEW1
TSGH 8301 NXPpS5pUVWmpcnH0bY9vKEG|c3H5 MV2yNEDDvU1? M4jQbVEhcA>? MlfPTY5kemWjc3XzJINmdGxibXnndoF1cW:w M3TUXVE6QDl4NEe1
Swiss3T3 NXj6dXhmS2:ub375MYZwem2rbnegRZN{[Xl? M1jhSVExKML3TR?= Mn\4NVMh\A>? MXLJcoNz\WG|ZYOgdJJwe3SjdHWgZ4VtdCClb3zvcpku\m:{bXnu[{Bi[3Srdnn0fS=> M3;BXlIyPDZ2OUCy
HT22 NXriO2JsS3m2b4TvfIlkKEG|c3H5 M4rqV|ExKML3TR?= NWDVR|JMOTNiaB?= MnfrVJJwfGWldIOgZYdicW6|dDDncJV1[W2jdHWtbY5lfWOnZDDu[ZVzd26jbDDk[YF1cA>? M{TTRlIzQDFyOEO1
Salivary gland stem cells MVPGeY5kfGmxbjDBd5NigQ>? NIfBPJUyOCEEtV2= MVm3JIQ> NVzi[5pDWmWmdXPld{BUT1OFIIPlcoV{[2WwY3W= MVWyOVgxPDV4MB?=

... 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:
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
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