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 MlrHSpVv[3Srb36gRZN{[Xl? NYD5c4FqOTBizszN M4TNN|IhcA>? MnzxSG1UVw>? NGHTcJFKdmirYnn0d{B1cGViYYPz[Y1jdHlib3[gcYlkem:2dXL1cIV{KGGwZDDpcpRmem2nZHnheIUh\mmuYX3lcpR{KHSxIH\vdo0h\Xi2ZX7k[YQheHKxY3Xzd4V{ NIm0Z5Y6PjR5NkW0
N1E-115 Mn3RSpVv[3Srb36gRZN{[Xl? NXqy[nNzOTBizszN NX:ySm9XOiCq MWfEUXNQ MYXJcohq[mm2czD0bIUh[XO|ZX3icJkhd2ZibXnjdo91fWK3bHXzJIFv\CCrboTldo1m\GmjdHWg[olt[W2nboTzJJRwKG[xcn2g[Zh1\W6mZXSgdJJw[2W|c3Xz NWr0NHloQTZ2N{[1OC=>
HeLa NXuzTnU{TnWwY4Tpc44hSXO|YYm= M2jJTlExKM7:TR?= MWGzNEBucW5? MknOTY5pcWKrdIOgeIhmKG[xcn3heIlwdiCxZjDzeJJme3NiZnni[ZJ{KGGwZDD0bIUh[XO|ZX3icJkhd2ZidnnuZ5VtcW5vY3;ueIFqdmmwZzDmc4NidCCjZHjld4lwdnN? M4n4TFk3PjhyN{K=
CCL39 MmP2SpVv[3Srb36gRZN{[Xl? M3Wyd|MxKM7:TR?= NF3YWG8{OCCvaX6= MnHVR49ueGyndHXsfUBi[m:uaYPo[ZMh[WO2aY\heIlwdiCxZjDOZU1JKGW6Y3jhcodmeiCQSFWxJIJ6KGmwdHXndolvew>? NYrSeVlHQTZ7M{O4Ni=>
Mesothelial cells from rat mesentery M{Sy[GlvfmG|aY\lJGF{e2G7 NYm3fmRsOzBizszN NF\DRo8zOCCq NY\SWXNtSmyxY3vzJIlvfmG|aY\lJIFkfGm4aYT5 MYK5PVMxQDd{
NIH3T3 M{LBTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPnNVAh|ryP MlfINVgh\A>? MWLEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To M2TyOVExODJzM{i2
Dbl-d Mo\0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXexNEDPxE1? NXH3Unl[OThiZB?= MXfTeJJwdmeueTDpcohq[mm2czDj[YxtKGe{b4f0bC=> MXOxNFAzOTN6Nh?=
Dbl-e MoX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVqxNEDPxE1? MUCxPEBl MkfMUY9l\XKjdHXsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MlHPNVAxOjF|OE[=
mNET1-d Ml;5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGiyc5IyOCEQvF2= MlzvNVgh\A>? M3fj[HN1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp MVWxNFAzOTN6Nh?=
mNET1-e NHXwcGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFKwfFkyOCEQvF2= NVfvSnFQOThiZB?= M4ra[3N1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp MWWxNFAzOTN6Nh?=
Ras-2 NWPLXXJoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWD1PWhsOTBizszN MUOxPEBl NVvqXYR3W3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh? M4\6NVExODJzM{i2
Ras-4 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPDNVAh|ryP Moq3NVgh\A>? NFS2O|dUfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NHHjS4QyODB{MUO4Oi=>
Src-1 NXfRNY5XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVqxNEDPxE1? MXuxPEBl MkmzSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> MXGxNFAzOTN6Nh?=
Src-4 NGnPVm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHLNVAh|ryP M3fRbVE5KGR? NEfCU3RFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp NGD6XmMyODB{MUO4Oi=>
NIH3T3 M1u1Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jDU|ExKM7:TR?= M3XWXFE5KGR? Mkf4SI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> MVyxNFAzOTN6Nh?=
Src-1 MmPwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLqNVAh|ryP MmKxNVgh\A>? NIm0fXpFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp NGe2PFQyODB{MUO4Oi=>
Src-2 MmP0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jqc|ExKM7:TR?= MXKxPEBl NEPWfHVFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp NFK1eFAyODB{MUO4Oi=>
SW620 NVKwdpVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXv1XWZSOTBizszN NUS5fplFOThiZB?= NX\yOoFuTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? MXexNFAzOTN6Nh?=
HCT15 M1:0Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnK2NVAh|ryP MXGxPEBl NWO4b3FITG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? MX[xNFAzOTN6Nh?=
HCT116 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\YOIFsOTBizszN M1z2WVE5KGR? NVjqXZB[W3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh? M3PXOVExODJzM{i2
LS174T NImwbZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1q1RVExKM7:TR?= M{DJd|E5KGR? NX\qOYpNVW:mZYLheIVtgSCrbnjpZol1eyClZXzsJIdzd3e2aB?= M2fC[VExODJzM{i2
Neonatal rat ventricular myocytes MYfGeY5kfGmxbjDBd5NigQ>? NFHHV5EyOCEQvF2= NU\6cVU5PDhiaB?= MWfJcohq[mm2czDFWE0yNWmwZIXj[YQhcW6lcnXhd4V{KGmwIIDyc5RmcW5ic4nueIhme2m|LDDj[YxtKHOrenWgZY5lKG27b3\pZpJqdGyjcjDvdodidmm8YYTpc44> NHvSOIcyODN6Nk[xNy=>
Stellate Cell MkOySpVv[3Srb36gRZN{[Xl? NUPIS|hTOjVizszN NUjvZoY2OTVibXnu NEK1bGdKdmirYnn0d{Bnd3KvYYTpc44hd2ZiRj3hZ5RqdiC|dILld5Mh\mmkZYLzJIFv\CCyaH;zdIhwenmuYYTpc44hd2ZibYnvd4lvKGyrZ3j0JINp[Wmw NV65T3dDOTB4MEC0PVY>
Rat Vascular Smooth Muscle Cells MWfGeY5kfGmxbjDBd5NigQ>? NInkepIyOCEQvF2= NFPs[GEzKGh? MWPJcohq[mm2czDhcodqd3SnboPpckBKUS2rbnT1Z4VlKGi7cHXyeJJweGi7 NUf1bWlTOTB4NEKzNVc>
PC3 M{nVVGZ2dmO2aX;uJGF{e2G7 Ml\aNlUh|ryP M3Xm[FEhcA>? NInINVFKdmS3Y3XzJI1wenCqb3zv[4lk[WxiY3jhcodmew>? NEHaXW8yODd{MES3NS=>
PC3 M1G2bG1q\3KjdHnvckBCe3OjeR?= MUmyOUDPxE1? MmXUNUBp NFHROYNKdmirYnn0d{B1cGViQl3GRk1EVSCjbnSgeIhmKEWJRj3zeIlufWyjdHXkJI1q\3KjdHnvci=> MlPZNVA4OjB2N{G=
PC3 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3niSlI2KM7:TR?= NVTEeohFOTdiaB?= MXvEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To M1rhWFExPzJyNEex
LNCaP M{\4NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTpb44zPSEQvF2= MorCNVchcA>? Ml\CSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> NH;oRpAyODd{MES3NS=>
Rat hepatic stellate cells NWnBNFlKTnWwY4Tpc44hSXO|YYm= MWmzNEDPxE1? NUfPb2RoPDhiaB?= NVLme|JmTGmvaX7pd4hmeyC2aHWgdIhwe3Cqb4L5cIF1cW:wIH;mJGVzczJuIHHu[EBl\WO{ZXHz[ZMhdmW5IFTORUB{gW62aHXzbZM> MV2xNFg1PTZ4Mx?=
Pancreatic acinar cells NYD1fFVITnWwY4Tpc44hSXO|YYm= NI\nVVMyOMLizszN M1\FSFcxKG2rbh?= NUPzbnRbWG:2ZX70bYF1\XNiQ1PLMZN1cW23bHH0[YQheGGwY4LlZZRq[yCnbor5cYUhe2WlcnX0bY9v MV[xNlc1PTB6MB?=
C2C12 MUDGeY5kfGmxbjDBd5NigQ>? NWftbFY4OTEEoN88US=> NGfDbIE3KGh? NFzDOnJRemW4ZX70d{B1cGVic3XybY5mKHCqb4PwbI9zgWyjdHnvckBw\iCLUmOtNUBqdmS3Y3XkJIJ6KGmwc4XsbY4h[W6mL3;yJHRPTi4QsR?= M{PPNVE3OjZ5MUK0
PC 12 MoGySpVv[3Srb36gRZN{[Xl? NUK1dnN2OTEEoN88US=> MWOyOEBp NX;UeXpzSXS2ZX71ZZRmeyClYYTlZ4hwdGGvaX7lJIJqd3O7boTo[ZNqew>? NW[w[5VUOTZ{MUm0NlQ>
Cynomolgus monkey embryonic stem cells M1TnZWN6fG:2b4jpZ{BCe3OjeR?= MmfYNlAhyrWP NH3peJEzPCCq NIDlRYhRem:vb4Tld{BkgUWVIHPlcIwhe3W{dnn2ZYw> MnvKNVg6PDB6NUW=
TSGH 8301 NI[wfmhOcWe{YYTpc44hSXO|YYm= M363RlIxKML3TR?= NGnWfZAyKGh? M2C1[Glv[3KnYYPld{Bk\WyuIH3p[5JifGmxbh?= M3fiZlE6QDl4NEe1
Swiss3T3 NVnCU4s2S2:ub375MYZwem2rbnegRZN{[Xl? M3:zXlExKML3TR?= MYmxN{Bl MkL0TY5kemWjc3XzJJBzd3O2YYTlJINmdGxiY3;sc456NW[xcn3pcoch[WO2aY\peJk> MnTCNlE1PjR7MEK=
HT22 MVrDfZRwfG:6aXOgRZN{[Xl? NEPKVJQyOCEEtV2= NVnNXZg6OTNiaB?= NH;wO3NRem:2ZXP0d{Bi\2GrboP0JIdtfXSjbXH0[U1qdmS3Y3XkJI5mfXKxbnHsJIRm[XSq MXeyNlgyODh|NR?=
Salivary gland stem cells NXn4V5FzTnWwY4Tpc44hSXO|YYm= MX6xNEDDvU1? MVy3JIQ> NUjjd3d[WmWmdXPld{BUT1OFIIPlcoV{[2WwY3W= M{nZWlI2QDB2NU[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 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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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

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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