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 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.

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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 M3vj[GZ2dmO2aX;uJGF{e2G7 M12xPFExKM7:TR?= NGflfJQzKGh? MlPTSG1UVw>? NVy5O41nUW6qaXLpeJMhfGinIHHzd4Vu[my7IH;mJI1q[3KxdIXieYxmeyCjbnSgbY51\XKvZXTpZZRmKG[rbHHt[Y51eyC2bzDmc5JuKGW6dHXu[IVlKHC{b3Pld5Nmew>? MkfJPVY1PzZ3NB?=
N1E-115 NF71TGdHfW6ldHnvckBCe3OjeR?= MV6xNEDPxE1? MoDvNkBp M4DtcWROW09? MmryTY5pcWKrdIOgeIhmKGG|c3XtZox6KG:oIH3pZ5JwfHWkdXzld{BidmRiaX70[ZJu\WSrYYTlJIZqdGGvZX70d{B1dyCob4LtJIV5fGWwZHXkJJBzd2Onc4Pldy=> MnKxPVY1PzZ3NB?=
HeLa M3q0dGZ2dmO2aX;uJGF{e2G7 MkPSNVAh|ryP NW[zfXhMOzBibXnu M2DNfmlvcGmkaYTzJJRp\SCob4LtZZRqd25ib3[gd5Rz\XO|IH\pZoVzeyCjbnSgeIhmKGG|c3XtZox6KG:oII\pcoN2dGmwLXPvcpRicW6rbneg[o9k[WxiYXTo[ZNqd26| NWn5SIdoQTZ4OEC3Ni=>
CCL39 MUDGeY5kfGmxbjDBd5NigQ>? NF\rXo8{OCEQvF2= MnS4N|AhdWmw NUX1OVQ2S2:vcHzleIVtgSCjYn;sbZNp\XNiYXP0bZZifGmxbjDv[kBP[S2KIHX4Z4hidmencjDOTGUyKGK7IHnueIVoemmwcx?= M1XkNVk3QTN|OEK=
Mesothelial cells from rat mesentery NYDOWGNlUW64YYPpeoUhSXO|YYm= NX\r[YZPOzBizszN NFz2VWozOCCq M{DUOmJtd2OtczDpcpZie2m4ZTDhZ5Rqfmm2eR?= NYXYXXd2QTl|MEi3Ni=>
NIH3T3 NVexRpA6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPOe25COTBizszN M1LJfVE5KGR? MX3Ec4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To MWWxNFAzOTN6Nh?=
Dbl-d MnvUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXexNEDPxE1? MXSxPEBl M1\HR3N1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp M3PrPVExODJzM{i2
Dbl-e NGXjNHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXFNVAh|ryP Mmf5NVgh\A>? NFXGT2lOd2SncnH0[Yx6KGmwaHnibZR{KGOnbHyg[5Jwf3Sq NFT6bJYyODB{MUO4Oi=>
mNET1-d MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PqSVExKM7:TR?= Mnv5NVgh\A>? NU\TV|V3W3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh? NWHycJp1OTByMkGzPFY>
mNET1-e MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoO1NVAh|ryP NHrUNIIyQCCm NH6ze5BUfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MnezNVAxOjF|OE[=
Ras-2 MkX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkGwNVAh|ryP MWCxPEBl M{PrPXN1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp MkXSNVAxOjF|OE[=
Ras-4 NUfqcZozT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWO2flBTOTBizszN NGTJN2IyQCCm NHi3XJFUfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NVXjZY1JOTByMkGzPFY>
Src-1 M4fWUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILmNVAyOCEQvF2= NVLYWWMxOThiZB?= NXrsbnBVTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? MV[xNFAzOTN6Nh?=
Src-4 Mo\BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\mNVAh|ryP MkjkNVgh\A>? MofTSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> NFnaNY4yODB{MUO4Oi=>
NIH3T3 NYfZNGFFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWSxNEDPxE1? MlzNNVgh\A>? MnnjSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> Mon6NVAxOjF|OE[=
Src-1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPSc5J1OTBizszN M{K5UVE5KGR? MlKySI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> MoiyNVAxOjF|OE[=
Src-2 M2m2[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTDNVAh|ryP MnjQNVgh\A>? NETkXnVFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp MUOxNFAzOTN6Nh?=
SW620 MojyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jXPVExKM7:TR?= NVLpXW52OThiZB?= M3;aZ2Rw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> NYiybnJPOTByMkGzPFY>
HCT15 Mn7mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXWxNEDPxE1? M2ezZlE5KGR? M2DTbGRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> NVS2RlZOOTByMkGzPFY>
HCT116 NHrC[3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXGwepJYOTBizszN NFH2eIIyQCCm NYLwcnRDW3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh? Mke1NVAxOjF|OE[=
LS174T MkD5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW[xNEDPxE1? NHLxSlAyQCCm MWHNc4RmemG2ZXz5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp NHT1TXUyODB{MUO4Oi=>
Neonatal rat ventricular myocytes MVnGeY5kfGmxbjDBd5NigQ>? NUOyUJluOTBizszN M3zZXVQ5KGh? MoPDTY5pcWKrdIOgSXQuOS2rbnT1Z4VlKGmwY4LlZZNmeyCrbjDwdo91\WmwIIP5cpRp\XOrczygZ4VtdCC|aYrlJIFv\CCveX;mbYJzcWyuYYKgc5Jo[W6renH0bY9v M2\4T|ExOzh4NkGz
Stellate Cell NV34OJdSTnWwY4Tpc44hSXO|YYm= MlW1NlUh|ryP NX\KcGtOOTVibXnu M3;tdWlvcGmkaYTzJIZwem2jdHnvckBw\iCILXHjeIlvKHO2cnXzd{BncWKncoOgZY5lKHCqb4PwbI9zgWyjdHnvckBw\iCveX;zbY4hdGmpaISgZ4hicW5? NXvjcmV3OTB4MEC0PVY>
Rat Vascular Smooth Muscle Cells MWHGeY5kfGmxbjDBd5NigQ>? NF7XWZIyOCEQvF2= MmWzNkBp Ml:1TY5pcWKrdIOgZY5ocW:2ZX7zbY4hUUlvaX7keYNm\CCqeYDldpRzd3CqeR?= MXKxNFY1OjNzNx?=
PC3 MVHGeY5kfGmxbjDBd5NigQ>? MnzvNlUh|ryP NGjxc|gyKGh? M1T4Smlv\HWlZYOgcY9zeGixbH;nbYNidCClaHHu[4V{ NU\KeIZUOTB5MkC0O|E>
PC3 MUPNbYdz[XSrb36gRZN{[Xl? NH;rTo0zPSEQvF2= MWOxJIg> NHK3b5BKdmirYnn0d{B1cGViQl3GRk1EVSCjbnSgeIhmKEWJRj3zeIlufWyjdHXkJI1q\3KjdHnvci=> NHXRTHMyODd{MES3NS=>
PC3 MnXBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlO3NlUh|ryP M{D4ZVE4KGh? NGT3WYVFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp NVvyelJwOTB5MkC0O|E>
LNCaP NXjWeWRqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M325cFI2KM7:TR?= NIPtTVkyPyCq NILwWYlFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp NFzGT|gyODd{MES3NS=>
Rat hepatic stellate cells MV\GeY5kfGmxbjDBd5NigQ>? NIro[Ic{OCEQvF2= NX\LSIV{PDhiaB?= M323fmRqdWmwaYPo[ZMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDFdoszNCCjbnSg[IVkemWjc3XzJI5mfyCGTlGgd5lvfGinc3nz NVPOWYN5OTB6NEW2OlM>
Pancreatic acinar cells NUf0OGdtTnWwY4Tpc44hSXO|YYm= M3XKWFExyqEQvF2= MXq3NEBucW5? M2XH[HBwfGWwdHnheIV{KEOFSz3zeIlufWyjdHXkJJBidmO{ZXH0bYMh\W68eX3lJJNm[3KndHnvci=> M4jzPVEzPzR3MEiw
C2C12 NIjyc2VHfW6ldHnvckBCe3OjeR?= MkDHNVDDqM7:TR?= M1nSZVYhcA>? NELONZFRemW4ZX70d{B1cGVic3XybY5mKHCqb4PwbI9zgWyjdHnvckBw\iCLUmOtNUBqdmS3Y3XkJIJ6KGmwc4XsbY4h[W6mL3;yJHRPTi4QsR?= MmTzNVYzPjdzMkS=
PC 12 NUjBflRkTnWwY4Tpc44hSXO|YYm= MXGxNOKh|ryP NIO5RpgzPCCq M{\GcWF1fGWwdXH0[ZMh[2G2ZXPoc4xidWmwZTDibY9{gW62aHXzbZM> M4fVNlE3OjF7NEK0
Cynomolgus monkey embryonic stem cells NGHYNGhEgXSxdH;4bYMhSXO|YYm= MkG0NlAhyrWP M2TOXVI1KGh? M2HMUHBzd22xdHXzJIN6TVNiY3XscEB{fXK4aY\hcC=> M3roZlE5QTRyOEW1
TSGH 8301 M1O1S21q\3KjdHnvckBCe3OjeR?= NF\0d3IzOCEEtV2= Ml;KNUBp MY\JcoNz\WG|ZYOgZ4VtdCCvaXfyZZRqd25? M3;sPFE6QDl4NEe1
Swiss3T3 MlywR49td267LX\vdo1qdmdiQYPzZZk> MXuxNEDDvU1? NFH5bVQyOyCm NWDGZYNyUW6lcnXhd4V{KHC{b4P0ZZRmKGOnbHygZ49td267LX\vdo1qdmdiYXP0bZZqfHl? NEjxfGIzOTR4NEmwNi=>
HT22 MYfDfZRwfG:6aXOgRZN{[Xl? NHKyPVQyOCEEtV2= MoexNVMhcA>? NXfMbYdIWHKxdHXjeJMh[WejaX7zeEBodHW2YX3heIUucW6mdXPl[EBv\XW{b37hcEBl\WG2aB?= MknZNlI5OTB6M{W=
Salivary gland stem cells NYi5fGtlTnWwY4Tpc44hSXO|YYm= NHK4PFAyOCEEtV2= Ml;HO{Bl M{fsXnJm\HWlZYOgV2dUSyC|ZX7ld4NmdmOn MmPVNlU5ODR3NkC=

... 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 individually and in order:
saline
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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID