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 NVW3flFHTnWwY4Tpc44hSXO|YYm= MVqxNEDPxE1? MWqyJIg> M1;VWmROW09? MX7Jcohq[mm2czD0bIUh[XO|ZX3icJkhd2ZibXnjdo91fWK3bHXzJIFv\CCrboTldo1m\GmjdHWg[olt[W2nboTzJJRwKG[xcn2g[Zh1\W6mZXSgdJJw[2W|c3Xz NWTTVXVuQTZ2N{[1OC=>
N1E-115 NV64dXZWTnWwY4Tpc44hSXO|YYm= NH3BflcyOCEQvF2= M3XmTFIhcA>? MmjlSG1UVw>? M1X3OmlvcGmkaYTzJJRp\SCjc4PlcYJtgSCxZjDtbYNzd3S3YoXs[ZMh[W6mIHnueIVzdWWmaXH0[UBncWyjbXXueJMhfG9iZn;ycUBmgHSnbnTl[EBxem:lZYPz[ZM> M1HuSVk3PDd4NUS=
HeLa NILxRWxHfW6ldHnvckBCe3OjeR?= MYCxNEDPxE1? MoLUN|AhdWmw NFrt[JVKdmirYnn0d{B1cGViZn;ycYF1cW:wIH;mJJN1emW|czDmbYJmenNiYX7kJJRp\SCjc4PlcYJtgSCxZjD2bY5kfWyrbj3jc451[WmwaX7nJIZw[2GuIHHkbIV{cW:wcx?= MoHIPVY3QDB5Mh?=
CCL39 M3;OSWZ2dmO2aX;uJGF{e2G7 M3nH[|MxKM7:TR?= NFLhRXE{OCCvaX6= MnP3R49ueGyndHXsfUBi[m:uaYPo[ZMh[WO2aY\heIlwdiCxZjDOZU1JKGW6Y3jhcodmeiCQSFWxJIJ6KGmwdHXndolvew>? MVi5Olk{Ozh{
Mesothelial cells from rat mesentery MUjJcpZie2m4ZTDBd5NigQ>? NHGzbFE{OCEQvF2= Mo\HNlAhcA>? MWnCcI9kc3NiaX72ZZNqfmViYXP0bZZqfHl? M{fIS|k6OzB6N{K=
NIH3T3 M{jYUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPMU2syOCEQvF2= NGjDN4wyQCCm NWfNUo52TG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? NXftVmR4OTByMkGzPFY>
Dbl-d M3zNXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4OyWVExKM7:TR?= M4OxZ|E5KGR? M{H0dnN1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp NETpdlgyODB{MUO4Oi=>
Dbl-e NIjUNJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWn0fIE5OTBizszN MlXnNVgh\A>? MmPSUY9l\XKjdHXsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NHTwUYkyODB{MUO4Oi=>
mNET1-d M4rrb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV:xNEDPxE1? NWr5U2d4OThiZB?= MVPTeJJwdmeueTDpcohq[mm2czDj[YxtKGe{b4f0bC=> NG\hWHgyODB{MUO4Oi=>
mNET1-e MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWWxNEDPxE1? M2fUe|E5KGR? MkLoV5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NUfzeZpPOTByMkGzPFY>
Ras-2 NULiNoVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1qzbFExKM7:TR?= MXOxPEBl M2TWWnN1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp NWjLZoNkOTByMkGzPFY>
Ras-4 Mmm3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHibXYyOCEQvF2= MoPaNVgh\A>? NX;mNXN7W3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh? MWqxNFAzOTN6Nh?=
Src-1 MkTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWexNEDPxE1? MU[xPEBl MojISI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> NXLwcmtkOTByMkGzPFY>
Src-4 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\2dlN[OTBizszN NV\SWGRJOThiZB?= M3T6OWRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> NHLwfGsyODB{MUO4Oi=>
NIH3T3 NWftVVVzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfYdJgyOCEQvF2= NXfmToRwOThiZB?= MV7Ec4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To MkO3NVAxOjF|OE[=
Src-1 NFXtWlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TDU|ExKM7:TR?= NYmzdFB3OThiZB?= NV3wUWlKTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? NFnvWZYyODB{MUO4Oi=>
Src-2 M1HS[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;PRXQyOCEQvF2= MU[xPEBl MX\Ec4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To NILXTlIyODB{MUO4Oi=>
SW620 NFLSfWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWGxNEDPxE1? M3f0ZlE5KGR? M3y1[mRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> MoLnNVAxOjF|OE[=
HCT15 M1;Ie2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvDZpMyOCEQvF2= NGDFd|gyQCCm M{W3OWRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> MWWxNFAzOTN6Nh?=
HCT116 NX;IUZk5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXyxNEDPxE1? M3rYXlE5KGR? M2[2R3N1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp M1fEclExODJzM{i2
LS174T NYfyNFdYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVWxNEDPxE1? MmrTNVgh\A>? MnK2UY9l\XKjdHXsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? M2fMPFExODJzM{i2
Neonatal rat ventricular myocytes M3;HXWZ2dmO2aX;uJGF{e2G7 MWKxNEDPxE1? NIq2[2s1QCCq NGKycXdKdmirYnn0d{BGXC1zLXnu[JVk\WRiaX7jdoVie2W|IHnuJJBzd3SnaX6gd5lvfGinc3nzMEBk\WyuIIPpfoUh[W6mIH35c4Zq[nKrbHzhdkBwemejbnn6ZZRqd25? NYrDfVVHOTB|OE[2NVM>
Stellate Cell NFu0bGRHfW6ldHnvckBCe3OjeR?= M2TzSVI2KM7:TR?= M1izSVE2KG2rbh?= MWrJcohq[mm2czDmc5Ju[XSrb36gc4YhTi2jY4TpckB{fHKnc4Og[olj\XK|IHHu[EBxcG:|cHjvdplt[XSrb36gc4YhdXmxc3nuJIxq\2i2IHPoZYlv NVLpfGM4OTB4MEC0PVY>
Rat Vascular Smooth Muscle Cells MoLpSpVv[3Srb36gRZN{[Xl? MWCxNEDPxE1? MnOxNkBp M33xUWlvcGmkaYTzJIFv\2mxdHXud4lvKEmLLXnu[JVk\WRiaInw[ZJ1em:yaIm= NYXlVZFoOTB4NEKzNVc>
PC3 MXHGeY5kfGmxbjDBd5NigQ>? MmTiNlUh|ryP M2GxUlEhcA>? MWXJcoR2[2W|IH3vdpBpd2yxZ3njZYwh[2ijbnfldy=> MWGxNFczODR5MR?=
PC3 NHT0c|JOcWe{YYTpc44hSXO|YYm= MUiyOUDPxE1? MlvENUBp NFLjN3FKdmirYnn0d{B1cGViQl3GRk1EVSCjbnSgeIhmKEWJRj3zeIlufWyjdHXkJI1q\3KjdHnvci=> MXqxNFczODR5MR?=
PC3 NHe4UZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rQ[|I2KM7:TR?= MXmxO{Bp M4Pp[mRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> Ml;iNVA4OjB2N{G=
LNCaP M1Tt[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXiN4duOjVizszN MXGxO{Bp MWDEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To Mm\VNVA4OjB2N{G=
Rat hepatic stellate cells MYnGeY5kfGmxbjDBd5NigQ>? M13T[FMxKM7:TR?= NGnROoU1QCCq MnTrSIlucW6rc3jld{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFXyb|ItKGGwZDDk[YNz\WG|ZYOgcoV4KESQQTDzfY51cGW|aYO= M3;ieVExQDR3Nk[z
Pancreatic acinar cells MVTGeY5kfGmxbjDBd5NigQ>? MkLwNVDDqM7:TR?= Mo\tO|AhdWmw NXXNeXVpWG:2ZX70bYF1\XNiQ1PLMZN1cW23bHH0[YQheGGwY4LlZZRq[yCnbor5cYUhe2WlcnX0bY9v M3znWlEzPzR3MEiw
C2C12 NITh[nZHfW6ldHnvckBCe3OjeR?= NUj2W2Z6OTEEoN88US=> NV[2dJdRPiCq NYq2[pNPWHKndnXueJMhfGinIIPldolv\SCyaH;zdIhwenmuYYTpc44hd2ZiSWLTMVEhcW6mdXPl[EBjgSCrboP1cIlvKGGwZD;vdkBVVkZvzsG= M4O5blE3OjZ5MUK0
PC 12 MW\GeY5kfGmxbjDBd5NigQ>? M{ThRlExyqEQvF2= MkTiNlQhcA>? MWHBeJRmdnWjdHXzJINifGWlaH;sZY1qdmViYnnvd5lvfGinc3nz MYmxOlIyQTR{NB?=
Cynomolgus monkey embryonic stem cells M1qyUWN6fG:2b4jpZ{BCe3OjeR?= NHnrNoQzOCEEtV2= MofDNlQhcA>? M4qxRnBzd22xdHXzJIN6TVNiY3XscEB{fXK4aY\hcC=> NWnud|gxOTh7NEC4OVU>
TSGH 8301 NXjCcIlTVWmpcnH0bY9vKEG|c3H5 NHm3W4MzOCEEtV2= NHzsOJkyKGh? NXT2cFNUUW6lcnXhd4V{KGOnbHygcYloemG2aX;u MkH5NVk5QTZ2N{W=
Swiss3T3 Ml61R49td267LX\vdo1qdmdiQYPzZZk> MUWxNEDDvU1? NFrkOZkyOyCm M3XXZ2lv[3KnYYPld{Bxem:|dHH0[UBk\WyuIHPvcI9vgS2ob4LtbY5oKGGldHn2bZR6 MUGyNVQ3PDlyMh?=
HT22 Ml;GR5l1d3SxeHnjJGF{e2G7 M{\ad|ExKML3TR?= NXzo[ZdPOTNiaB?= M36wT3Bzd3SnY4TzJIFo[Wmwc4Sg[4x2fGGvYYTlMYlv\HWlZXSgcoV2em:wYXyg[IVifGh? Mn63NlI5OTB6M{W=
Salivary gland stem cells M1PDNmZ2dmO2aX;uJGF{e2G7 NVPl[INzOTBiwsXN MVq3JIQ> M4Lre3Jm\HWlZYOgV2dUSyC|ZX7ld4NmdmOn MWiyOVgxPDV4MB?=

... 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
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