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 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 M2HTcGZ2dmO2aX;uJGF{e2G7 M{fBOVExKM7:TR?= NYDrenRJOiCq MWPEUXNQ MX;Jcohq[mm2czD0bIUh[XO|ZX3icJkhd2ZibXnjdo91fWK3bHXzJIFv\CCrboTldo1m\GmjdHWg[olt[W2nboTzJJRwKG[xcn2g[Zh1\W6mZXSgdJJw[2W|c3Xz NIeyXWI6PjR5NkW0
N1E-115 NUn6VHBKTnWwY4Tpc44hSXO|YYm= NIPIbGUyOCEQvF2= MnnqNkBp NWfLe4ZMTE2VTx?= NXn2XGllUW6qaXLpeJMhfGinIHHzd4Vu[my7IH;mJI1q[3KxdIXieYxmeyCjbnSgbY51\XKvZXTpZZRmKG[rbHHt[Y51eyC2bzDmc5JuKGW6dHXu[IVlKHC{b3Pld5Nmew>? NXfqVY5DQTZ2N{[1OC=>
HeLa MULGeY5kfGmxbjDBd5NigQ>? NGnmSYgyOCEQvF2= Mm\hN|AhdWmw MYrJcohq[mm2czD0bIUh\m:{bXH0bY9vKG:oIIP0doV{eyCoaXLldpMh[W6mIITo[UBie3OnbXLsfUBw\iC4aX7jeYxqdi2lb370ZYlvcW6pIH\vZ4FtKGGmaHXzbY9vew>? MVe5OlY5ODd{
CCL39 M2jZVWZ2dmO2aX;uJGF{e2G7 NFKzWo0{OCEQvF2= MmrWN|AhdWmw MXrDc41xdGW2ZXz5JIFjd2yrc3jld{Bi[3SrdnH0bY9vKG:oIF7hMWgh\XilaHHu[4VzKE6KRUGgZpkhcW62ZXfybY5{ NIL1UmM6Pjl|M{iy
Mesothelial cells from rat mesentery MV7JcpZie2m4ZTDBd5NigQ>? MoPDN|Ah|ryP M17z[lIxKGh? M1\rUmJtd2OtczDpcpZie2m4ZTDhZ5Rqfmm2eR?= NV21XZZrQTl|MEi3Ni=>
NIH3T3 NXrjdmIzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXENVAh|ryP M13yNVE5KGR? MXTEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To NXGyWmlVOTByMkGzPFY>
Dbl-d NIO1Nm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDJNVAh|ryP MWexPEBl MoD0V5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg> M1XmV|ExODJzM{i2
Dbl-e NX;teY9MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3L2SVExKM7:TR?= MXuxPEBl NH\vRppOd2SncnH0[Yx6KGmwaHnibZR{KGOnbHyg[5Jwf3Sq MWKxNFAzOTN6Nh?=
mNET1-d NWrBWWN7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUGxNEDPxE1? Mnq0NVgh\A>? M{OyXnN1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp NF7iW|AyODB{MUO4Oi=>
mNET1-e MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvmNVAh|ryP NIHyW3MyQCCm NF\WepVUfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MVqxNFAzOTN6Nh?=
Ras-2 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLlcI5mOTBizszN NGXScmcyQCCm M4S1SHN1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp NUPvOHo4OTByMkGzPFY>
Ras-4 MmizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVixNEDPxE1? MmLBNVgh\A>? NYjucFJNW3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh? MlHSNVAxOjF|OE[=
Src-1 NYPISlhVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLBcGYyOCEQvF2= NHPmb4cyQCCm NYLaOHdkTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? MoLnNVAxOjF|OE[=
Src-4 M2nWTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7kZmYyOCEQvF2= NVvifpJJOThiZB?= M{PRemRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> MoHBNVAxOjF|OE[=
NIH3T3 MoTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlG0NVAh|ryP M{ToelE5KGR? M2nIdmRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> NYDmWnhsOTByMkGzPFY>
Src-1 NUjzdFNvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrJS4IyOCEQvF2= NHS1ZZcyQCCm MXTEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To NFrjOoMyODB{MUO4Oi=>
Src-2 MlnyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY[5SnJbOTBizszN M3LkbFE5KGR? NHz1UVlFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp MUOxNFAzOTN6Nh?=
SW620 NGTITWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHji[XkyOCEQvF2= MVGxPEBl Ml;tSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> NI\Qe3oyODB{MUO4Oi=>
HCT15 M2Tacmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFS4SJoyOCEQvF2= MWixPEBl NHvSUFJFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp NWD6dGszOTByMkGzPFY>
HCT116 NF63XZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVyxNEDPxE1? NEC0dWEyQCCm NXjPdodFW3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh? MljPNVAxOjF|OE[=
LS174T MorxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDlbJQyOCEQvF2= MVuxPEBl NETXN4hOd2SncnH0[Yx6KGmwaHnibZR{KGOnbHyg[5Jwf3Sq M2HIfFExODJzM{i2
Neonatal rat ventricular myocytes M1PQcGZ2dmO2aX;uJGF{e2G7 NVvWWol1OTBizszN NU\VSHNRPDhiaB?= NYjFNJZSUW6qaXLpeJMhTVRvMT3pcoR2[2WmIHnuZ5Jm[XOnczDpckBxem:2ZXnuJJN6dnSqZYPpd{wh[2WubDDzbZpmKGGwZDDtfY9ncWK{aXzsZZIhd3KpYX7pfoF1cW:w NFTwbGkyODN6Nk[xNy=>
Stellate Cell M{jLZWZ2dmO2aX;uJGF{e2G7 MmKwNlUh|ryP NXzrUmp5OTVibXnu M3HyOWlvcGmkaYTzJIZwem2jdHnvckBw\iCILXHjeIlvKHO2cnXzd{BncWKncoOgZY5lKHCqb4PwbI9zgWyjdHnvckBw\iCveX;zbY4hdGmpaISgZ4hicW5? M4q3[lExPjByNEm2
Rat Vascular Smooth Muscle Cells M3PtbGZ2dmO2aX;uJGF{e2G7 MoCwNVAh|ryP NX3aUJhFOiCq NHjZO2xKdmirYnn0d{Bidmerb4TlcpNqdiCLST3pcoR2[2WmIHj5dIVzfHKxcHj5 Mki0NVA3PDJ|MUe=
PC3 NIL0VVhHfW6ldHnvckBCe3OjeR?= MX[yOUDPxE1? NV7vWWVVOSCq NFjNUZlKdmS3Y3XzJI1wenCqb3zv[4lk[WxiY3jhcodmew>? MWKxNFczODR5MR?=
PC3 M4fqeW1q\3KjdHnvckBCe3OjeR?= NYjsTHdyOjVizszN NXvGd2F{OSCq MYTJcohq[mm2czD0bIUhSk2IQj3DUUBidmRidHjlJGVITi2|dHnteYxifGWmIH3p[5JifGmxbh?= NEG5XGgyODd{MES3NS=>
PC3 M2PPOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLoNlUh|ryP NHKzXGkyPyCq NGq4VZlFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp MVWxNFczODR5MR?=
LNCaP Mn7vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1r2c|I2KM7:TR?= NI\ZVYYyPyCq MV;Ec4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To NVvWVIhNOTB5MkC0O|E>
Rat hepatic stellate cells NFHoUGZHfW6ldHnvckBCe3OjeR?= MYqzNEDPxE1? NGX1[ZE1QCCq NEf5UXFFcW2rbnnzbIV{KHSqZTDwbI9{eGixconsZZRqd25ib3[gSZJsOixiYX7kJIRm[3KnYYPld{Bv\XdiRF7BJJN6dnSqZYPpdy=> Mn;VNVA5PDV4NkO=
Pancreatic acinar cells NIj1O|FHfW6ldHnvckBCe3OjeR?= M1jMXlExyqEQvF2= NEGwe404OCCvaX6= MYHQc5RmdnSrYYTld{BES0tvc4TpcZVt[XSnZDDwZY5kemWjdHnjJIVvgnmvZTDz[YNz\XSrb36= Mnr1NVI4PDVyOEC=
C2C12 MlrqSpVv[3Srb36gRZN{[Xl? NWHaXFJSOTEEoN88US=> M3XBT|YhcA>? Ml3yVJJmfmWwdIOgeIhmKHOncnnu[UBxcG:|cHjvdplt[XSrb36gc4YhUVKVLUGgbY5lfWOnZDDifUBqdnO3bHnuJIFv\C:xcjDUUmYu|rF? NYmwS2dkOTZ{NkexNlQ>
PC 12 M3LxS2Z2dmO2aX;uJGF{e2G7 NVTlW3p7OTEEoN88US=> M{jy[|I1KGh? NFfGe5dCfHSnboXheIV{KGOjdHXjbI9t[W2rbnWgZolwe3mwdHjld4l{ M1rnblE3OjF7NEK0
Cynomolgus monkey embryonic stem cells Mn\sR5l1d3SxeHnjJGF{e2G7 MoX1NlAhyrWP M2jIXVI1KGh? Mmi5VJJwdW:2ZYOgZ5lGWyClZXzsJJN2en[rdnHs M3PDPFE5QTRyOEW1
TSGH 8301 MknNUYloemG2aX;uJGF{e2G7 M4\NT|IxKML3TR?= M{\0U|EhcA>? M3i2bWlv[3KnYYPld{Bk\WyuIH3p[5JifGmxbh?= NVzvfph3OTl6OU[0O|U>
Swiss3T3 MWfDc4xwdnlvZn;ycYlv\yCDc4PhfS=> MmjoNVAhyrWP NH\EfHoyOyCm Mm[yTY5kemWjc3XzJJBzd3O2YYTlJINmdGxiY3;sc456NW[xcn3pcoch[WO2aY\peJk> MWmyNVQ3PDlyMh?=
HT22 M3vEcGN6fG:2b4jpZ{BCe3OjeR?= M3fKdFExKML3TR?= MUGxN{Bp MYTQdo91\WO2czDh[4FqdnO2IHfseZRidWG2ZT3pcoR2[2WmIH7leZJwdmGuIHTlZZRp NF2xfnkzOjhzMEizOS=>
Salivary gland stem cells MmnUSpVv[3Srb36gRZN{[Xl? MXmxNEDDvU1? M{PvWlch\A>? M4fu[XJm\HWlZYOgV2dUSyC|ZX7ld4NmdmOn M1vPcVI2QDB2NU[w

... 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