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.

Size Price Stock Quantity  
In DMSO USD 156 In stock
USD 70 In stock
USD 120 In stock
USD 170 In stock
USD 570 In stock

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Cited by 45 Publications

4 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.

    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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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 NWPGNY5[TnWwY4Tpc44hSXO|YYm= NWDSVldROTBizszN NHy3R5AzKGh? MVLEUXNQ MX7Jcohq[mm2czD0bIUh[XO|ZX3icJkhd2ZibXnjdo91fWK3bHXzJIFv\CCrboTldo1m\GmjdHWg[olt[W2nboTzJJRwKG[xcn2g[Zh1\W6mZXSgdJJw[2W|c3Xz MVy5OlQ4PjV2
N1E-115 NWPHeHNwTnWwY4Tpc44hSXO|YYm= NGDSWZcyOCEQvF2= NGn1dpgzKGh? NHLwfHZFVVOR NIPjSHNKdmirYnn0d{B1cGViYYPz[Y1jdHlib3[gcYlkem:2dXL1cIV{KGGwZDDpcpRmem2nZHnheIUh\mmuYX3lcpR{KHSxIH\vdo0h\Xi2ZX7k[YQheHKxY3Xzd4V{ Mn3QPVY1PzZ3NB?=
HeLa NFmxSYdHfW6ldHnvckBCe3OjeR?= NUHjUJVyOTBizszN M1PDSlMxKG2rbh?= M4TpXmlvcGmkaYTzJJRp\SCob4LtZZRqd25ib3[gd5Rz\XO|IH\pZoVzeyCjbnSgeIhmKGG|c3XtZox6KG:oII\pcoN2dGmwLXPvcpRicW6rbneg[o9k[WxiYXTo[ZNqd26| MYC5OlY5ODd{
CCL39 MlfRSpVv[3Srb36gRZN{[Xl? NUP6T3VGOzBizszN M{j5cFMxKG2rbh?= NYryd4JDS2:vcHzleIVtgSCjYn;sbZNp\XNiYXP0bZZifGmxbjDv[kBP[S2KIHX4Z4hidmencjDOTGUyKGK7IHnueIVoemmwcx?= NWnkN|RSQTZ7M{O4Ni=>
Mesothelial cells from rat mesentery NYfhVpRlUW64YYPpeoUhSXO|YYm= MVSzNEDPxE1? MW[yNEBp NHrtco1DdG:la4OgbY53[XOrdnWgZYN1cX[rdIm= MVW5PVMxQDd{
NIH3T3 M{DTfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mne0NVAh|ryP NIHWTHIyQCCm NInPbHRFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp NGPk[JoyODB{MUO4Oi=>
Dbl-d NGDPcYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzFfJQyOCEQvF2= NYj3TnhvOThiZB?= MmDvV5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg> M2DPWVExODJzM{i2
Dbl-e NX3FWGlWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3TNVAh|ryP M3fEcVE5KGR? M2LZTm1w\GW{YYTlcJkhcW6qaXLpeJMh[2WubDDndo94fGh? M2[x[FExODJzM{i2
mNET1-d NUnwfFY1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\4SVExKM7:TR?= NHzEdm4yQCCm NUj5ZYNIW3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh? NGLZSmYyODB{MUO4Oi=>
mNET1-e MnHCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\vV5RROTBizszN MU[xPEBl MnL4V5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg> M4rpXlExODJzM{i2
Ras-2 NIe1TpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TpUVExKM7:TR?= NV7Ve5lZOThiZB?= Mn\MV5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MYWxNFAzOTN6Nh?=
Ras-4 NFW1botIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVX4T5dHOTBizszN MWKxPEBl MUnTeJJwdmeueTDpcohq[mm2czDj[YxtKGe{b4f0bC=> NH\NUmMyODB{MUO4Oi=>
Src-1 NVX0N2VlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWj3b5JjOTBizszN NYfNSmVLOThiZB?= NWrSZ|lJTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? MVOxNFAzOTN6Nh?=
Src-4 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPN[Wh[OTBizszN NVPzPHBYOThiZB?= MVXEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To NIOxcWwyODB{MUO4Oi=>
NIH3T3 NIPZdVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;VcFhCOTBizszN MUWxPEBl NGKx[lFFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp NUHjcoVjOTByMkGzPFY>
Src-1 MlvKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfjNVAh|ryP M1;DVlE5KGR? NWfLc5JiTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? NEj5OpEyODB{MUO4Oi=>
Src-2 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDmNVAh|ryP M1K4WlE5KGR? NUCyXnhYTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? NUD6SoZDOTByMkGzPFY>
SW620 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nBUFExKM7:TR?= M3ntWVE5KGR? MY\Ec4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To MoXlNVAxOjF|OE[=
HCT15 NV7RTm1VT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4i1eVExKM7:TR?= M{nLVFE5KGR? NHvaOJJFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp MWmxNFAzOTN6Nh?=
HCT116 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTZXo9POTBizszN NWXNN3BDOThiZB?= MmP4V5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MV:xNFAzOTN6Nh?=
LS174T NX21PGZTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MomzNVAh|ryP M132Z|E5KGR? NHfoXHNOd2SncnH0[Yx6KGmwaHnibZR{KGOnbHyg[5Jwf3Sq M3nGNlExODJzM{i2
Neonatal rat ventricular myocytes NYnIWW53TnWwY4Tpc44hSXO|YYm= NXLWPWtYOTBizszN NHvoV241QCCq NHniN|RKdmirYnn0d{BGXC1zLXnu[JVk\WRiaX7jdoVie2W|IHnuJJBzd3SnaX6gd5lvfGinc3nzMEBk\WyuIIPpfoUh[W6mIH35c4Zq[nKrbHzhdkBwemejbnn6ZZRqd25? NFr3RoIyODN6Nk[xNy=>
Stellate Cell NInM[XJHfW6ldHnvckBCe3OjeR?= NV;td3FMOjVizszN M17ROFE2KG2rbh?= NVLZR|VyUW6qaXLpeJMh\m:{bXH0bY9vKG:oIF[tZYN1cW5ic4Ty[ZN{KG[rYnXyd{BidmRicHjvd5Bpd3K7bHH0bY9vKG:oIH35c5NqdiCuaXfoeEBkcGGrbh?= Mn6wNVA3ODB2OU[=
Rat Vascular Smooth Muscle Cells MXjGeY5kfGmxbjDBd5NigQ>? MkDYNVAh|ryP MWmyJIg> NX75XZlCUW6qaXLpeJMh[W6paX;0[Y5{cW5iSVmtbY5lfWOnZDDofZBmenS{b4DofS=> NIDQZXYyODZ2MkOxOy=>
PC3 MWrGeY5kfGmxbjDBd5NigQ>? MUmyOUDPxE1? NYfoNFZ7OSCq Mor0TY5lfWOnczDtc5JxcG:ub3fpZ4FtKGOqYX7n[ZM> Ml;mNVA4OjB2N{G=
PC3 M1K0ZW1q\3KjdHnvckBCe3OjeR?= Mn3WNlUh|ryP Ml35NUBp NXfXfFBRUW6qaXLpeJMhfGinIFLNSmIuS01iYX7kJJRp\SCHR1[td5RqdXWuYYTl[EBucWe{YYTpc44> M3fvbVExPzJyNEex
PC3 NIm0SZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHtNIszPSEQvF2= MlnZNVchcA>? MorYSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> NV7zW|A{OTB5MkC0O|E>
LNCaP MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTPNlUh|ryP NXXIZpVbOTdiaB?= NIHWWWpFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp MnPENVA4OjB2N{G=
Rat hepatic stellate cells M{HLWGZ2dmO2aX;uJGF{e2G7 MVKzNEDPxE1? MoewOFghcA>? NVGy[4dJTGmvaX7pd4hmeyC2aHWgdIhwe3Cqb4L5cIF1cW:wIH;mJGVzczJuIHHu[EBl\WO{ZXHz[ZMhdmW5IFTORUB{gW62aHXzbZM> M4\WSlExQDR3Nk[z
Pancreatic acinar cells M2izcmZ2dmO2aX;uJGF{e2G7 NGPFfXoyOMLizszN M2r0OlcxKG2rbh?= M{fIW3BwfGWwdHnheIV{KEOFSz3zeIlufWyjdHXkJJBidmO{ZXH0bYMh\W68eX3lJJNm[3KndHnvci=> M33BdVEzPzR3MEiw
C2C12 Mom1SpVv[3Srb36gRZN{[Xl? NXv5bZRvOTEEoN88US=> NHP0O2I3KGh? MWrQdoV3\W62czD0bIUhe2W{aX7lJJBpd3OyaH;yfYxifGmxbjDv[kBKWlNvMTDpcoR2[2WmIHL5JIlve3WuaX6gZY5lN2:{IGTOSk3PuQ>? M1rZcFE3OjZ5MUK0
PC 12 MoT6SpVv[3Srb36gRZN{[Xl? NW\PelhvOTEEoN88US=> Mn;jNlQhcA>? MVXBeJRmdnWjdHXzJINifGWlaH;sZY1qdmViYnnvd5lvfGinc3nz MmP0NVYzOTl2MkS=
Cynomolgus monkey embryonic stem cells NHfTSWVEgXSxdH;4bYMhSXO|YYm= MUKyNEDDvU1? MnHwNlQhcA>? NX3UeXBWWHKxbX;0[ZMh[3mHUzDj[YxtKHO3co\peoFt Mnj6NVg6PDB6NUW=
TSGH 8301 NH;BWG9OcWe{YYTpc44hSXO|YYm= MXqyNEDDvU1? MV:xJIg> M2exbGlv[3KnYYPld{Bk\WyuIH3p[5JifGmxbh?= NXX1RlBOOTl6OU[0O|U>
Swiss3T3 NE\Le3lEd2yxbomt[o9zdWmwZzDBd5NigQ>? M{izT|ExKML3TR?= NV7zOZFYOTNiZB?= M1S3cGlv[3KnYYPld{Bxem:|dHH0[UBk\WyuIHPvcI9vgS2ob4LtbY5oKGGldHn2bZR6 NFH3SIczOTR4NEmwNi=>
HT22 MUXDfZRwfG:6aXOgRZN{[Xl? NWDhUFU4OTBiwsXN NWrFbVh6OTNiaB?= M{n4OHBzd3SnY4TzJIFo[Wmwc4Sg[4x2fGGvYYTlMYlv\HWlZXSgcoV2em:wYXyg[IVifGh? MmfFNlI5OTB6M{W=
Salivary gland stem cells M1\jVmZ2dmO2aX;uJGF{e2G7 M3jyZlExKML3TR?= MkTRO{Bl M{PUbXJm\HWlZYOgV2dUSyC|ZX7ld4NmdmOn NYPDXm55OjV6MES1OlA>

... 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 (199.83 mM) warming
Water 14 mg/mL (43.71 mM)
Ethanol <1 mg/mL
In vivo Saline 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID