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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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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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 M4fxV2Z2dmO2aX;uJGF{e2G7 MoixNVAh|ryP MlLnNkBp MXzEUXNQ NXPJPVdVUW6qaXLpeJMhfGinIHHzd4Vu[my7IH;mJI1q[3KxdIXieYxmeyCjbnSgbY51\XKvZXTpZZRmKG[rbHHt[Y51eyC2bzDmc5JuKGW6dHXu[IVlKHC{b3Pld5Nmew>? NF\CSWc6PjR5NkW0
N1E-115 M3K2d2Z2dmO2aX;uJGF{e2G7 NWGzNHVEOTBizszN MVmyJIg> MX\EUXNQ MlPYTY5pcWKrdIOgeIhmKGG|c3XtZox6KG:oIH3pZ5JwfHWkdXzld{BidmRiaX70[ZJu\WSrYYTlJIZqdGGvZX70d{B1dyCob4LtJIV5fGWwZHXkJJBzd2Onc4Pldy=> NUP6VHVZQTZ2N{[1OC=>
HeLa MnvnSpVv[3Srb36gRZN{[Xl? MmnvNVAh|ryP NF\xWFg{OCCvaX6= M3zhfWlvcGmkaYTzJJRp\SCob4LtZZRqd25ib3[gd5Rz\XO|IH\pZoVzeyCjbnSgeIhmKGG|c3XtZox6KG:oII\pcoN2dGmwLXPvcpRicW6rbneg[o9k[WxiYXTo[ZNqd26| MVu5OlY5ODd{
CCL39 MUnGeY5kfGmxbjDBd5NigQ>? NV3OTXV3OzBizszN MnrlN|AhdWmw MmfjR49ueGyndHXsfUBi[m:uaYPo[ZMh[WO2aY\heIlwdiCxZjDOZU1JKGW6Y3jhcodmeiCQSFWxJIJ6KGmwdHXndolvew>? MV25Olk{Ozh{
Mesothelial cells from rat mesentery MYTJcpZie2m4ZTDBd5NigQ>? M1zpOVMxKM7:TR?= MoHzNlAhcA>? MXTCcI9kc3NiaX72ZZNqfmViYXP0bZZqfHl? MW[5PVMxQDd{
NIH3T3 NIjjNpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPKeFZ1OTBizszN MofTNVgh\A>? NFj5T29Fd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp MkG5NVAxOjF|OE[=
Dbl-d MnXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfSSmsyOCEQvF2= NFK2PFgyQCCm NWDiUJBjW3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh? NYjJbVM6OTByMkGzPFY>
Dbl-e NGOzVZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVu5WJk3OTBizszN M2\IXlE5KGR? MXrNc4RmemG2ZXz5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp MYexNFAzOTN6Nh?=
mNET1-d MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXOxNEDPxE1? MYSxPEBl MYLTeJJwdmeueTDpcohq[mm2czDj[YxtKGe{b4f0bC=> M3:2[lExODJzM{i2
mNET1-e NIDWb4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\YRlExKM7:TR?= MoPUNVgh\A>? MVHTeJJwdmeueTDpcohq[mm2czDj[YxtKGe{b4f0bC=> M33CelExODJzM{i2
Ras-2 Mn7VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU[xNEDPxE1? NIXtb4oyQCCm MlLaV5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NIW5N4wyODB{MUO4Oi=>
Ras-4 NI\6fItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDMN3QyOCEQvF2= M2rnWlE5KGR? Mn3oV5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NGPqOoIyODB{MUO4Oi=>
Src-1 Mnr2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TUOlExKM7:TR?= NG\LNXgyQCCm NX;MWmJXTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? NY\3eIJ{OTByMkGzPFY>
Src-4 NGW3epZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnDdm8xOTBizszN M3LGXVE5KGR? MWjEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To Mk\kNVAxOjF|OE[=
NIH3T3 NVPZdo94T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrPOGZoOTBizszN Ml;SNVgh\A>? M4\ERmRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> NF32b5AyODB{MUO4Oi=>
Src-1 M2PON2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rYTVExKM7:TR?= M1;G[FE5KGR? MlXwSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> Mo\ZNVAxOjF|OE[=
Src-2 M3rKfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrnNVAh|ryP M1flUFE5KGR? M4PxZ2Rw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> MYKxNFAzOTN6Nh?=
SW620 NWnNb4JCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\aVGJUOTBizszN MlvtNVgh\A>? NUHvXngxTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? NGTTd4IyODB{MUO4Oi=>
HCT15 MlqwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGC0N3UyOCEQvF2= M33iV|E5KGR? M{DBNGRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> MVSxNFAzOTN6Nh?=
HCT116 M{jS[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vSflExKM7:TR?= Mmr3NVgh\A>? NVPMRopYW3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh? MoroNVAxOjF|OE[=
LS174T NXLEPYNxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzKe3gyOCEQvF2= MnjpNVgh\A>? NH7pPWNOd2SncnH0[Yx6KGmwaHnibZR{KGOnbHyg[5Jwf3Sq NH\STlkyODB{MUO4Oi=>
Neonatal rat ventricular myocytes NHLhR4dHfW6ldHnvckBCe3OjeR?= MVGxNEDPxE1? MoDvOFghcA>? MkLqTY5pcWKrdIOgSXQuOS2rbnT1Z4VlKGmwY4LlZZNmeyCrbjDwdo91\WmwIIP5cpRp\XOrczygZ4VtdCC|aYrlJIFv\CCveX;mbYJzcWyuYYKgc5Jo[W6renH0bY9v MUGxNFM5PjZzMx?=
Stellate Cell M3X1N2Z2dmO2aX;uJGF{e2G7 MUiyOUDPxE1? NF7a[40yPSCvaX6= MUnJcohq[mm2czDmc5Ju[XSrb36gc4YhTi2jY4TpckB{fHKnc4Og[olj\XK|IHHu[EBxcG:|cHjvdplt[XSrb36gc4YhdXmxc3nuJIxq\2i2IHPoZYlv MorQNVA3ODB2OU[=
Rat Vascular Smooth Muscle Cells M33x[2Z2dmO2aX;uJGF{e2G7 NYfpNIV6OTBizszN MWeyJIg> MlHlTY5pcWKrdIOgZY5ocW:2ZX7zbY4hUUlvaX7keYNm\CCqeYDldpRzd3CqeR?= M333U|ExPjR{M{G3
PC3 Mm\tSpVv[3Srb36gRZN{[Xl? NVTvNm9HOjVizszN NU\SVWdCOSCq NFzieI9KdmS3Y3XzJI1wenCqb3zv[4lk[WxiY3jhcodmew>? M2[5R|ExPzJyNEex
PC3 NVn4SJpFVWmpcnH0bY9vKEG|c3H5 NYK2XZNxOjVizszN Mo\0NUBp NX3VbVFCUW6qaXLpeJMhfGinIFLNSmIuS01iYX7kJJRp\SCHR1[td5RqdXWuYYTl[EBucWe{YYTpc44> MUOxNFczODR5MR?=
PC3 M3\oUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mni1NlUh|ryP Mn3ENVchcA>? NXr3bW9HTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? MmnzNVA4OjB2N{G=
LNCaP NG\0fmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVmyOUDPxE1? NGDQW5AyPyCq MkTxSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> MkHuNVA4OjB2N{G=
Rat hepatic stellate cells NYHB[XF{TnWwY4Tpc44hSXO|YYm= MVSzNEDPxE1? NIKwPYk1QCCq MWLEbY1qdmm|aHXzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRYLrNkwh[W6mIHTlZ5Jm[XOnczDu[ZchTE6DIIP5cpRp\XOrcx?= M2PDZlExQDR3Nk[z
Pancreatic acinar cells NIDR[FhHfW6ldHnvckBCe3OjeR?= MVWxNOKh|ryP NV;6b4VCPzBibXnu MYHQc5RmdnSrYYTld{BES0tvc4TpcZVt[XSnZDDwZY5kemWjdHnjJIVvgnmvZTDz[YNz\XSrb36= MXGxNlc1PTB6MB?=
C2C12 NIKwdmVHfW6ldHnvckBCe3OjeR?= MkjuNVDDqM7:TR?= NGXGOFQ3KGh? NUn0d3RqWHKndnXueJMhfGinIIPldolv\SCyaH;zdIhwenmuYYTpc44hd2ZiSWLTMVEhcW6mdXPl[EBjgSCrboP1cIlvKGGwZD;vdkBVVkZvzsG= M{L4XVE3OjZ5MUK0
PC 12 NUe0coRjTnWwY4Tpc44hSXO|YYm= Mn61NVDDqM7:TR?= M3LtW|I1KGh? MnzwRZR1\W63YYTld{Bk[XSnY3jvcIFucW6nIHLpc5N6dnSqZYPpdy=> M3vmVlE3OjF7NEK0
Cynomolgus monkey embryonic stem cells NHn3bW5EgXSxdH;4bYMhSXO|YYm= MmDZNlAhyrWP MVyyOEBp M2DqdXBzd22xdHXzJIN6TVNiY3XscEB{fXK4aY\hcC=> M{jlO|E5QTRyOEW1
TSGH 8301 M{fvNm1q\3KjdHnvckBCe3OjeR?= MnzCNlAhyrWP MmLCNUBp NEjrTVZKdmO{ZXHz[ZMh[2WubDDtbYdz[XSrb36= M1i2O|E6QDl4NEe1
Swiss3T3 Ml:0R49td267LX\vdo1qdmdiQYPzZZk> NI\yb4IyOCEEtV2= NUnzRZRFOTNiZB?= NUPWc3N3UW6lcnXhd4V{KHC{b4P0ZZRmKGOnbHygZ49td267LX\vdo1qdmdiYXP0bZZqfHl? NFnlbnYzOTR4NEmwNi=>
HT22 M3q3SGN6fG:2b4jpZ{BCe3OjeR?= MVWxNEDDvU1? NE[1R5UyOyCq M2DQWXBzd3SnY4TzJIFo[Wmwc4Sg[4x2fGGvYYTlMYlv\HWlZXSgcoV2em:wYXyg[IVifGh? M2TZOVIzQDFyOEO1
Salivary gland stem cells MlTjSpVv[3Srb36gRZN{[Xl? NVXC[WgyOTBiwsXN MnHSO{Bl MWDS[YR2[2W|IGPHV2Mhe2WwZYPj[Y5k\Q>? M37E[FI2QDB2NU[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
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