Y-27632 2HCl

Catalog No.S1049

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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Y-27632 2HCl Chemical Structure

Y-27632 2HCl Chemical Structure
Molecular Weight: 320.26

Validation & Quality Control

Cited by 45 publications:

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  • Research Area
  • Inhibition Profile
  • Y-27632 2HCl Mechanism
  • Combination Therapy
    Combination Therapy

Product Description

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)
IC50 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
Swiss 3T3 cellsNH;jN3VHfW6ldHnvckBCe3OjeR?=NGGyT3QyOCEQvF2=NHX0clYzKGh?NFrTSJBFVVORNYjWWnFSUW6qaXLpeJMhfGinIHHzd4Vu[my7IH;mJI1q[3KxdIXieYxmeyCjbnSgbY51\XKvZXTpZZRmKG[rbHHt[Y51eyC2bzDmc5JuKGW6dHXu[IVlKHC{b3Pld5Nmew>?NHn2SXA6PjR5NkW0
N1E-115NVHSZo9QTnWwY4Tpc44hSXO|YYm=NH72XoUyOCEQvF2=M1L3ZlIhcA>?MUXEUXNQNXruUXN6UW6qaXLpeJMhfGinIHHzd4Vu[my7IH;mJI1q[3KxdIXieYxmeyCjbnSgbY51\XKvZXTpZZRmKG[rbHHt[Y51eyC2bzDmc5JuKGW6dHXu[IVlKHC{b3Pld5Nmew>?NFvlc2Y6PjR5NkW0
HeLaMkm4SpVv[3Srb36gRZN{[Xl?NF71WnEyOCEQvF2=NE\FZlQ{OCCvaX6=MmH1TY5pcWKrdIOgeIhmKG[xcn3heIlwdiCxZjDzeJJme3NiZnni[ZJ{KGGwZDD0bIUh[XO|ZX3icJkhd2ZidnnuZ5VtcW5vY3;ueIFqdmmwZzDmc4NidCCjZHjld4lwdnN?MVy5OlY5ODd{
CCL39NG\5TohHfW6ldHnvckBCe3OjeR?=MUKzNEDPxE1?MnPTN|AhdWmwM4izTGNwdXCuZYTlcJkh[WKxbHnzbIV{KGGldHn2ZZRqd25ib3[gUoEuUCCneHPoZY5o\XJiTljFNUBjgSCrboTl[5JqdnN?NXHHd2Y6QTZ7M{O4Ni=>
Mesothelial cells from rat mesenteryNFjPWWdKdn[jc3n2[UBCe3OjeR?=M3HzTlMxKM7:TR?=NVXaU4g5OjBiaB?=NELGe5RDdG:la4OgbY53[XOrdnWgZYN1cX[rdIm=MXy5PVMxQDd{
NIH3T3NYLLWHpIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MXuxNEDPxE1?NXvSd2s6OThiZB?=NH63NI5Fd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5RpMn;mNVAxOjF|OE[=
Dbl-dM13aTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M1PtTFExKM7:TR?=NVzyfGhjOThiZB?=MXXTeJJwdmeueTDpcohq[mm2czDj[YxtKGe{b4f0bC=>Ml;uNVAxOjF|OE[=
Dbl-eNITCO5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NXvWVYVNOTBizszNM4LjWlE5KGR?NFjNNVVOd2SncnH0[Yx6KGmwaHnibZR{KGOnbHyg[5Jwf3SqNFzjbVcyODB{MUO4Oi=>
mNET1-dM{DwcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NUflUYFWOTBizszNNXPzd4N2OThiZB?=M1\yVXN1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5RpNHjYPWIyODB{MUO4Oi=>
mNET1-eMlXvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NEP4XZkyOCEQvF2=M2HlfFE5KGR?M3TpZXN1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5RpM3rCWFExODJzM{i2
Ras-2Mor2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NUf5[|hkOTBizszNMm\KNVgh\A>?NYjrd2t3W3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh?MlyzNVAxOjF|OE[=
Ras-4M1PyeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MVyxNEDPxE1?NFr5e48yQCCmM3n6[XN1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5RpM4nhXlExODJzM{i2
Src-1M{nnVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NWnyUY1zOTBizszNM1;SR|E5KGR?NIKwNndFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5RpMl30NVAxOjF|OE[=
Src-4NGXuO2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M1va[|ExKM7:TR?=NVTIOIRoOThiZB?=NXrxUFF3TG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>?MkLJNVAxOjF|OE[=
NIH3T3NYq1b5JrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MXixNEDPxE1?NX20[YJzOThiZB?=MYDEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4ToNUSzWpRkOTByMkGzPFY>
Src-1M12zNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7Mn\sNVAh|ryPNF7JTpMyQCCmM37udmRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg>NW[zUWtQOTByMkGzPFY>
Src-2MlLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NHrpfXkyOCEQvF2=MV6xPEBlMkn5SI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=>MYqxNFAzOTN6Nh?=
SW620NYDHXIxHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NGfhfZQyOCEQvF2=MnPnNVgh\A>?NUewcWI5TG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>?NGG3VFMyODB{MUO4Oi=>
HCT15NHrF[oxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MkPnNVAh|ryPNXHoPJpZOThiZB?=NGqzSldFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5RpNXS2R41lOTByMkGzPFY>
HCT116NFLscHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MmjYNVAh|ryPMnHlNVgh\A>?NG\JSWdUfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>?NVWyU|JDOTByMkGzPFY>
LS174TM3Kye2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7M{T6[FExKM7:TR?=M1LzXVE5KGR?NV\QU216VW:mZYLheIVtgSCrbnjpZol1eyClZXzsJIdzd3e2aB?=NXrhZYJOOTByMkGzPFY>
Neonatal rat ventricular myocytesNXyydG1QTnWwY4Tpc44hSXO|YYm=M4XZUFExKM7:TR?=NGHtUZA1QCCqNYf3fI9NUW6qaXLpeJMhTVRvMT3pcoR2[2WmIHnuZ5Jm[XOnczDpckBxem:2ZXnuJJN6dnSqZYPpd{wh[2WubDDzbZpmKGGwZDDtfY9ncWK{aXzsZZIhd3KpYX7pfoF1cW:wMXexNFM5PjZzMx?=
Stellate CellNV;6SGh1TnWwY4Tpc44hSXO|YYm=NH;VR3kzPSEQvF2=NFfNXngyPSCvaX6=NFn4[lZKdmirYnn0d{Bnd3KvYYTpc44hd2ZiRj3hZ5RqdiC|dILld5Mh\mmkZYLzJIFv\CCyaH;zdIhwenmuYYTpc44hd2ZibYnvd4lvKGyrZ3j0JINp[WmwM1;nWlExPjByNEm2
Rat Vascular Smooth Muscle CellsNWHVO256TnWwY4Tpc44hSXO|YYm=MWCxNEDPxE1?NUPZXlc6OiCqM3jsNmlvcGmkaYTzJIFv\2mxdHXud4lvKEmLLXnu[JVk\WRiaInw[ZJ1em:yaIm=Mm\uNVA3PDJ|MUe=
PC3NGjoN4xHfW6ldHnvckBCe3OjeR?=NH7hUXYzPSEQvF2=NWHlZZB{OSCqNWD2d2FMUW6mdXPld{Bud3KyaH;sc4dq[2GuIHPoZY5o\XN?NH[yUGMyODd{MES3NS=>
PC3M2nFOW1q\3KjdHnvckBCe3OjeR?=MUiyOUDPxE1?M2\hR|EhcA>?MnvmTY5pcWKrdIOgeIhmKEKPRlKtR20h[W6mIITo[UBGT0Zvc4TpcZVt[XSnZDDtbYdz[XSrb36=NVPKXG05OTB5MkC0O|E>
PC3M2\RTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NITLNGszPSEQvF2=NYjmfJk4OTdiaB?=M3XHZmRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg>M3mxPFExPzJyNEex
LNCaPM17MbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7Mmr2NlUh|ryPM4XNOVE4KGh?M1n5XWRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg>MWWxNFczODR5MR?=
Rat hepatic stellate cellsNUD1eJRbTnWwY4Tpc44hSXO|YYm=MWezNEDPxE1?NWfZWmtDPDhiaB?=MVrEbY1qdmm|aHXzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRYLrNkwh[W6mIHTlZ5Jm[XOnczDu[ZchTE6DIIP5cpRp\XOrcx?=MXOxNFg1PTZ4Mx?=
Pancreatic acinar cellsMX\GeY5kfGmxbjDBd5NigQ>?Mn7lNVDDqM7:TR?=MXW3NEBucW5?M1fUW3BwfGWwdHnheIV{KEOFSz3zeIlufWyjdHXkJJBidmO{ZXH0bYMh\W68eX3lJJNm[3KndHnvci=>Mn31NVI4PDVyOEC=
C2C12MlG3SpVv[3Srb36gRZN{[Xl?MmPENVDDqM7:TR?=NHXtSJQ3KGh?M2HhdXBz\X[nboTzJJRp\SC|ZYLpcoUheGixc4Doc5J6dGG2aX;uJI9nKEmUUz2xJIlv\HWlZXSgZpkhcW6|dXzpckBidmRxb4KgWG5HNc7zNVvHbIdmOTZ{NkexNlQ>
PC 12MnHYSpVv[3Srb36gRZN{[Xl?MlTLNVDDqM7:TR?=M2H3dlI1KGh?MX7BeJRmdnWjdHXzJINifGWlaH;sZY1qdmViYnnvd5lvfGinc3nzNHnSeZoyPjJzOUSyOC=>
Cynomolgus monkey embryonic stem cellsNWjFVldWS3m2b4TvfIlkKEG|c3H5NHHjdGEzOCEEtV2=M4jQ[|I1KGh?MoX2VJJwdW:2ZYOgZ5lGWyClZXzsJJN2en[rdnHsNHfHfWEyQDl2MEi1OS=>
TSGH 8301MXPNbYdz[XSrb36gRZN{[Xl?MViyNEDDvU1?MXixJIg>NHn4SVVKdmO{ZXHz[ZMh[2WubDDtbYdz[XSrb36=M{LiTVE6QDl4NEe1
Swiss3T3MXvDc4xwdnlvZn;ycYlv\yCDc4PhfS=>MX:xNEDDvU1?NFLqfVAyOyCmNYPXdFRUUW6lcnXhd4V{KHC{b4P0ZZRmKGOnbHygZ49td267LX\vdo1qdmdiYXP0bZZqfHl?NUfLN4dxOjF2NkS5NFI>
HT22NVfSXpBzS3m2b4TvfIlkKEG|c3H5M4P2TVExKML3TR?=MkTPNVMhcA>?NUTKbYtlWHKxdHXjeJMh[WejaX7zeEBodHW2YX3heIUucW6mdXPl[EBv\XW{b37hcEBl\WG2aB?=MUiyNlgyODh|NR?=
Salivary gland stem cellsNE\xWHNHfW6ldHnvckBCe3OjeR?=MWmxNEDDvU1?MYe3JIQ>Mn;VVoVlfWOnczDTS3NEKHOnbnXzZ4Vv[2V?MVmyOVgxPDV4MB?=

... 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]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

Phosphorylation reactions The p160ROCK is expressed in COS cells as tagged full-length proteins, and immunoprecipitated by the use of anti-tag antibodies. The p160ROCK (30 ng) is incubated with 40 μM [γ-32P]ATP (3.3 Ci/mmol) and with 3 μg of either histone (HF2A), dephosphorylated casein or MBP in the presence of various concentrations of Y-27632 2HCl at 30 °C in a total volume of 31 μL. A 7 μL aliquot is taken at 0, 5, 10, and 20 minutes, mixed with an equal volume of 2 × Laemmli sample buffer, and applied to SDS-PAGE. The gel is stained with Commassie Blue, dried and subjected to analysis by a Bioimage Analyzer BAS2000. The Y-27632 2HCl concentration required to inhibit p160ROCK activity by 50% (IC50 value) is obtained. Ki value is calculated according to the equation, Ki = IC50/(1 + S/Km), where S and Km represent concentrations of and Km value for ATP.

Animal Study: [1] [7]

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)

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Uehata M, et al. Nature, 1997, 389(6654), 990-994.

[2] Itoh K, et al. Nat Med, 1999, 5(2), 221-225.

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Chemical Information

Download Y-27632 2HCl SDF
Molecular Weight (MW) 320.26
Formula

C14H21N3O.2HCl

CAS No. 129830-38-2
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 64 mg/mL warming (199.83 mM)
Water 14 mg/mL (43.71 mM)
Ethanol <1 mg/mL (<1 mM)
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 Name (1R,4r)-4-((R)-1-aminoethyl)-N-(pyridin-4-yl)cyclohexanecarboxamide dihydrochloride

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.

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.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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