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
USD 70 In stock
USD 120 In stock
USD 170 In stock
USD 570 In stock

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Cited by 46 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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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 NI[2[IFHfW6ldHnvckBCe3OjeR?= NUnsSY4zOTBizszN MYeyJIg> NX[xO3pDTE2VTx?= NX;jSXVnUW6qaXLpeJMhfGinIHHzd4Vu[my7IH;mJI1q[3KxdIXieYxmeyCjbnSgbY51\XKvZXTpZZRmKG[rbHHt[Y51eyC2bzDmc5JuKGW6dHXu[IVlKHC{b3Pld5Nmew>? NVvuVlhnQTZ2N{[1OC=>
N1E-115 NH3DXIFHfW6ldHnvckBCe3OjeR?= MlXaNVAh|ryP Ml30NkBp NWHHSplGTE2VTx?= MoCzTY5pcWKrdIOgeIhmKGG|c3XtZox6KG:oIH3pZ5JwfHWkdXzld{BidmRiaX70[ZJu\WSrYYTlJIZqdGGvZX70d{B1dyCob4LtJIV5fGWwZHXkJJBzd2Onc4Pldy=> M4ntW|k3PDd4NUS=
HeLa M1y5N2Z2dmO2aX;uJGF{e2G7 M{CwSVExKM7:TR?= MXezNEBucW5? NHXQUYVKdmirYnn0d{B1cGViZn;ycYF1cW:wIH;mJJN1emW|czDmbYJmenNiYX7kJJRp\SCjc4PlcYJtgSCxZjD2bY5kfWyrbj3jc451[WmwaX7nJIZw[2GuIHHkbIV{cW:wcx?= M2jjUlk3PjhyN{K=
CCL39 M135VGZ2dmO2aX;uJGF{e2G7 NEPtb4M{OCEQvF2= MV2zNEBucW5? M1LPS2NwdXCuZYTlcJkh[WKxbHnzbIV{KGGldHn2ZZRqd25ib3[gUoEuUCCneHPoZY5o\XJiTljFNUBjgSCrboTl[5JqdnN? MYm5Olk{Ozh{
Mesothelial cells from rat mesentery NWPnTHVnUW64YYPpeoUhSXO|YYm= NEfBTYI{OCEQvF2= Mn7qNlAhcA>? MmjYRoxw[2u|IHnueoF{cX[nIHHjeIl3cXS7 Mlj0PVk{ODh5Mh?=
NIH3T3 NGrxb|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX[xNEDPxE1? MorvNVgh\A>? M2PjOGRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> NIf3bFkyODB{MUO4Oi=>
Dbl-d MlvqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTKOGgyOCEQvF2= M{HWV|E5KGR? M1O3THN1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp MWGxNFAzOTN6Nh?=
Dbl-e MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTwNZlTOTBizszN MVWxPEBl MVjNc4RmemG2ZXz5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp MUmxNFAzOTN6Nh?=
mNET1-d NYnrN4FFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;5RVgyOCEQvF2= NXvW[XRoOThiZB?= MkXZV5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MX[xNFAzOTN6Nh?=
mNET1-e NFqxVlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3ZNVAh|ryP M2jGXVE5KGR? M3rzR3N1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp MlmxNVAxOjF|OE[=
Ras-2 MlL1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;o[lExKM7:TR?= NUnGfXl2OThiZB?= NHzH[I5UfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MmfGNVAxOjF|OE[=
Ras-4 MoKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV[xeGRjOTBizszN MWqxPEBl NITpUo5UfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MUixNFAzOTN6Nh?=
Src-1 Mnj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWixNEDPxE1? NELUV5AyQCCm MlnPSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> M4\PNlExODJzM{i2
Src-4 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnI[Y1OOTBizszN NFfJRoQyQCCm MkX5SI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> MXGxNFAzOTN6Nh?=
NIH3T3 MnHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTxNVAh|ryP MYCxPEBl M4HJ[2Rw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> NXLPZ|BIOTByMkGzPFY>
Src-1 NEPTXWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTB[JpKOTBizszN NFixbo0yQCCm NELGN4xFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp MVmxNFAzOTN6Nh?=
Src-2 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTDNY0yOCEQvF2= M2PMe|E5KGR? Ml7rSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> M{fjU|ExODJzM{i2
SW620 M3;vS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXu3UopVOTBizszN NHLhWnoyQCCm MoC0SI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> MVyxNFAzOTN6Nh?=
HCT15 NE\pe4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\nbppxOTBizszN MlPQNVgh\A>? MXXEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To M2izcVExODJzM{i2
HCT116 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY[xNEDPxE1? M3m4VlE5KGR? M4\oUnN1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp M{CxflExODJzM{i2
LS174T MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\nVGROOTBizszN MkTuNVgh\A>? NVTpUZFlVW:mZYLheIVtgSCrbnjpZol1eyClZXzsJIdzd3e2aB?= MUKxNFAzOTN6Nh?=
Neonatal rat ventricular myocytes M2jvPGZ2dmO2aX;uJGF{e2G7 NUXJc25COTBizszN MYW0PEBp NIH5XndKdmirYnn0d{BGXC1zLXnu[JVk\WRiaX7jdoVie2W|IHnuJJBzd3SnaX6gd5lvfGinc3nzMEBk\WyuIIPpfoUh[W6mIH35c4Zq[nKrbHzhdkBwemejbnn6ZZRqd25? NVf0NpJ1OTB|OE[2NVM>
Stellate Cell NIHmPZJHfW6ldHnvckBCe3OjeR?= NGWzbIgzPSEQvF2= MmX4NVUhdWmw NVvZVlJmUW6qaXLpeJMh\m:{bXH0bY9vKG:oIF[tZYN1cW5ic4Ty[ZN{KG[rYnXyd{BidmRicHjvd5Bpd3K7bHH0bY9vKG:oIH35c5NqdiCuaXfoeEBkcGGrbh?= MYexNFYxODR7Nh?=
Rat Vascular Smooth Muscle Cells MU\GeY5kfGmxbjDBd5NigQ>? M{PBcFExKM7:TR?= MX:yJIg> NYXUdJd3UW6qaXLpeJMh[W6paX;0[Y5{cW5iSVmtbY5lfWOnZDDofZBmenS{b4DofS=> NFO4[JMyODZ2MkOxOy=>
PC3 MoHrSpVv[3Srb36gRZN{[Xl? NWPE[lIxOjVizszN NETibYIyKGh? NIrJXYdKdmS3Y3XzJI1wenCqb3zv[4lk[WxiY3jhcodmew>? NU\5R5pXOTB5MkC0O|E>
PC3 MnTBUYloemG2aX;uJGF{e2G7 NVXUXotyOjVizszN MVexJIg> M2nOU2lvcGmkaYTzJJRp\SCETV\CMWNOKGGwZDD0bIUhTUeILYP0bY12dGG2ZXSgcYloemG2aX;u NH7hcVgyODd{MES3NS=>
PC3 NVTHNIVyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmL6NlUh|ryP MXexO{Bp M3jaUWRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> MlqzNVA4OjB2N{G=
LNCaP MmPhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TiUVI2KM7:TR?= MUCxO{Bp MWrEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To M3LES|ExPzJyNEex
Rat hepatic stellate cells MXzGeY5kfGmxbjDBd5NigQ>? MlfmN|Ah|ryP NV3hVG5FPDhiaB?= NHPmcJpFcW2rbnnzbIV{KHSqZTDwbI9{eGixconsZZRqd25ib3[gSZJsOixiYX7kJIRm[3KnYYPld{Bv\XdiRF7BJJN6dnSqZYPpdy=> NEfN[IYyODh2NU[2Ny=>
Pancreatic acinar cells MXLGeY5kfGmxbjDBd5NigQ>? Mne5NVDDqM7:TR?= MVO3NEBucW5? NWP1WXRFWG:2ZX70bYF1\XNiQ1PLMZN1cW23bHH0[YQheGGwY4LlZZRq[yCnbor5cYUhe2WlcnX0bY9v MXixNlc1PTB6MB?=
C2C12 M3i1bWZ2dmO2aX;uJGF{e2G7 MkHGNVDDqM7:TR?= NYPHbXFiPiCq NWfGRnY4WHKndnXueJMhfGinIIPldolv\SCyaH;zdIhwenmuYYTpc44hd2ZiSWLTMVEhcW6mdXPl[EBjgSCrboP1cIlvKGGwZD;vdkBVVkZvzsG= M4DublE3OjZ5MUK0
PC 12 M2OzdWZ2dmO2aX;uJGF{e2G7 MmjsNVDDqM7:TR?= NFviRoczPCCq MnjRRZR1\W63YYTld{Bk[XSnY3jvcIFucW6nIHLpc5N6dnSqZYPpdy=> MWOxOlIyQTR{NB?=
Cynomolgus monkey embryonic stem cells MYTDfZRwfG:6aXOgRZN{[Xl? MYiyNEDDvU1? NHf6ZZYzPCCq MWXQdo9ud3SnczDjfWVUKGOnbHygd5Vzfmm4YXy= MonLNVg6PDB6NUW=
TSGH 8301 NEfiOIJOcWe{YYTpc44hSXO|YYm= MnrlNlAhyrWP MlXQNUBp NYLYcHBNUW6lcnXhd4V{KGOnbHygcYloemG2aX;u M1LWW|E6QDl4NEe1
Swiss3T3 NWDrZVAyS2:ub375MYZwem2rbnegRZN{[Xl? NXPTOHNoOTBiwsXN NFfjZowyOyCm MkLRTY5kemWjc3XzJJBzd3O2YYTlJINmdGxiY3;sc456NW[xcn3pcoch[WO2aY\peJk> M{Gzd|IyPDZ2OUCy
HT22 M4LS[mN6fG:2b4jpZ{BCe3OjeR?= MkDPNVAhyrWP MV[xN{Bp Mne2VJJwfGWldIOgZYdicW6|dDDncJV1[W2jdHWtbY5lfWOnZDDu[ZVzd26jbDDk[YF1cA>? NX\RUHNVOjJ6MUC4N|U>
Salivary gland stem cells Mn;HSpVv[3Srb36gRZN{[Xl? MWCxNEDDvU1? NHrjT2M4KGR? NIT3WJFT\WS3Y3XzJHNIW0Nic3Xu[ZNk\W6lZR?= NYnCV|VyOjV6MES1OlA>

... 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 <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