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 53 Publications

6 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.

    At day 8, cells were replated onto Matrigel-coated Transwell membranes at 106 cells/cm2 in the presence or absence of 10 mM Y-27632. TEER was measured at day 10, 2 days after replating.

    Science, 2017, 3(11):e1701679. 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.

    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.

  • 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.

    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 M4T4SmZ2dmO2aX;uJGF{e2G7 NHv3UHgyOCEQvF2= MWKyJIg> M{HT[2ROW09? MnHYTY5pcWKrdIOgeIhmKGG|c3XtZox6KG:oIH3pZ5JwfHWkdXzld{BidmRiaX70[ZJu\WSrYYTlJIZqdGGvZX70d{B1dyCob4LtJIV5fGWwZHXkJJBzd2Onc4Pldy=> M4Ljblk3PDd4NUS=
N1E-115 NIfnSVZHfW6ldHnvckBCe3OjeR?= NWLuVGRbOTBizszN M3OwU|IhcA>? Mni0SG1UVw>? NXvCdXdTUW6qaXLpeJMhfGinIHHzd4Vu[my7IH;mJI1q[3KxdIXieYxmeyCjbnSgbY51\XKvZXTpZZRmKG[rbHHt[Y51eyC2bzDmc5JuKGW6dHXu[IVlKHC{b3Pld5Nmew>? NF3Rfpc6PjR5NkW0
HeLa NWjRdVN7TnWwY4Tpc44hSXO|YYm= NV;pToZ5OTBizszN Mn3pN|AhdWmw MXTJcohq[mm2czD0bIUh\m:{bXH0bY9vKG:oIIP0doV{eyCoaXLldpMh[W6mIITo[UBie3OnbXLsfUBw\iC4aX7jeYxqdi2lb370ZYlvcW6pIH\vZ4FtKGGmaHXzbY9vew>? M2rCSFk3PjhyN{K=
CCL39 NHS2Z4NHfW6ldHnvckBCe3OjeR?= NYPRV4o6OzBizszN NEO0bHc{OCCvaX6= MWTDc41xdGW2ZXz5JIFjd2yrc3jld{Bi[3SrdnH0bY9vKG:oIF7hMWgh\XilaHHu[4VzKE6KRUGgZpkhcW62ZXfybY5{ Mo\TPVY6OzN6Mh?=
Mesothelial cells from rat mesentery NVXqfWNWUW64YYPpeoUhSXO|YYm= MYGzNEDPxE1? NXjmXZNnOjBiaB?= MVzCcI9kc3NiaX72ZZNqfmViYXP0bZZqfHl? NFyxT2w6QTNyOEey
NIH3T3 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjvN4RoOTBizszN MXOxPEBl MmDDSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> MVexNFAzOTN6Nh?=
Dbl-d NHmwTIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzMNVAh|ryP NH;CZlgyQCCm MnHnV5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg> Mk[2NVAxOjF|OE[=
Dbl-e MlHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlv1NVAh|ryP NH;VVVAyQCCm MmPpUY9l\XKjdHXsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MVqxNFAzOTN6Nh?=
mNET1-d Mk\JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfnNVAh|ryP MV[xPEBl M3;V[HN1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp NHewd|cyODB{MUO4Oi=>
mNET1-e NXjyRWtXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUKxNEDPxE1? MlvRNVgh\A>? NFvBVFRUfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NUDOVGpkOTByMkGzPFY>
Ras-2 Mlu5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVqxNEDPxE1? NHSzVoQyQCCm NXvQPFlRW3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh? MkTXNVAxOjF|OE[=
Ras-4 Ml3SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13pRlExKM7:TR?= NUeySWxjOThiZB?= M{f1PHN1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp NEfEfHEyODB{MUO4Oi=>
Src-1 M2XPe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfReYR7OTBizszN MnnYNVgh\A>? NXzs[HM5TG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? NYe2Wmh5OTByMkGzPFY>
Src-4 NXrqUmNIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nWblExKM7:TR?= MkXUNVgh\A>? Ml30SI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> M2PVOlExODJzM{i2
NIH3T3 M{W4bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nuTlExKM7:TR?= MoLpNVgh\A>? NVLVc3FKTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? NV[5O|B3OTByMkGzPFY>
Src-1 NXX0UFlDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVKxNEDPxE1? MWqxPEBl M{DaTGRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> M4\5OlExODJzM{i2
Src-2 NVfHfWFmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWexNEDPxE1? MWSxPEBl NW\vdJRqTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? MoXFNVAxOjF|OE[=
SW620 Mm\SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXmPJIyOCEQvF2= NU\Fb25LOThiZB?= MV;Ec4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To M4r5eFExODJzM{i2
HCT15 M{nJV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fzT|ExKM7:TR?= MljmNVgh\A>? Mn;LSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> MUKxNFAzOTN6Nh?=
HCT116 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PieFExKM7:TR?= M2q3blE5KGR? MYDTeJJwdmeueTDpcohq[mm2czDj[YxtKGe{b4f0bC=> NIjKSJMyODB{MUO4Oi=>
LS174T NWjQbXFtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfnNVAh|ryP NUTvbWVlOThiZB?= MmnBUY9l\XKjdHXsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MmfCNVAxOjF|OE[=
Neonatal rat ventricular myocytes M1O1XmZ2dmO2aX;uJGF{e2G7 MY[xNEDPxE1? NXzkdoZMPDhiaB?= M1vQcGlvcGmkaYTzJGVVNTFvaX7keYNm\CCrbnPy[YF{\XNiaX6gdJJwfGWrbjDzfY51cGW|aYOsJINmdGxic3n6[UBidmRibYnv[oljemmubHHyJI9z\2GwaYrheIlwdg>? MX6xNFM5PjZzMx?=
Stellate Cell NVnzW5hJTnWwY4Tpc44hSXO|YYm= M2fLXVI2KM7:TR?= NHn6b5IyPSCvaX6= NX60VGJpUW6qaXLpeJMh\m:{bXH0bY9vKG:oIF[tZYN1cW5ic4Ty[ZN{KG[rYnXyd{BidmRicHjvd5Bpd3K7bHH0bY9vKG:oIH35c5NqdiCuaXfoeEBkcGGrbh?= NE\yZWsyODZyMES5Oi=>
Rat Vascular Smooth Muscle Cells M1;jeWZ2dmO2aX;uJGF{e2G7 NIDCcWIyOCEQvF2= MYKyJIg> M{PXPWlvcGmkaYTzJIFv\2mxdHXud4lvKEmLLXnu[JVk\WRiaInw[ZJ1em:yaIm= M1WzXlExPjR{M{G3
PC3 NIjsWoZHfW6ldHnvckBCe3OjeR?= MUSyOUDPxE1? Ml32NUBp MUXJcoR2[2W|IH3vdpBpd2yxZ3njZYwh[2ijbnfldy=> M4rBNFExPzJyNEex
PC3 NW\1emF1VWmpcnH0bY9vKEG|c3H5 NXfxU3NFOjVizszN NEPNWW0yKGh? NUH6bWs2UW6qaXLpeJMhfGinIFLNSmIuS01iYX7kJJRp\SCHR1[td5RqdXWuYYTl[EBucWe{YYTpc44> MkHRNVA4OjB2N{G=
PC3 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzXRYQzPSEQvF2= M1zKTVE4KGh? Ml;6SI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> NYez[FZWOTB5MkC0O|E>
LNCaP MmLNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWWyOUDPxE1? MnXQNVchcA>? NV7Cc2RNTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? M2\OclExPzJyNEex
Rat hepatic stellate cells M3rxXWZ2dmO2aX;uJGF{e2G7 NYL2NFE{OzBizszN M33oUVQ5KGh? NHfPUpNFcW2rbnnzbIV{KHSqZTDwbI9{eGixconsZZRqd25ib3[gSZJsOixiYX7kJIRm[3KnYYPld{Bv\XdiRF7BJJN6dnSqZYPpdy=> M2fLPVExQDR3Nk[z
Pancreatic acinar cells NInUVnFHfW6ldHnvckBCe3OjeR?= MYGxNOKh|ryP M2PBT|cxKG2rbh?= MUHQc5RmdnSrYYTld{BES0tvc4TpcZVt[XSnZDDwZY5kemWjdHnjJIVvgnmvZTDz[YNz\XSrb36= NF;DcZAyOjd2NUC4NC=>
C2C12 NEW5T3hHfW6ldHnvckBCe3OjeR?= M2PafFExyqEQvF2= MWS2JIg> NXy1WWpHWHKndnXueJMhfGinIIPldolv\SCyaH;zdIhwenmuYYTpc44hd2ZiSWLTMVEhcW6mdXPl[EBjgSCrboP1cIlvKGGwZD;vdkBVVkZvzsG= NEDOeYsyPjJ4N{GyOC=>
PC 12 MWXGeY5kfGmxbjDBd5NigQ>? M33xcVExyqEQvF2= MXGyOEBp M3HHPGF1fGWwdXH0[ZMh[2G2ZXPoc4xidWmwZTDibY9{gW62aHXzbZM> MY[xOlIyQTR{NB?=
Cynomolgus monkey embryonic stem cells MnjNR5l1d3SxeHnjJGF{e2G7 Ml;uNlAhyrWP Mnv2NlQhcA>? MoTzVJJwdW:2ZYOgZ5lGWyClZXzsJJN2en[rdnHs M3zO[|E5QTRyOEW1
TSGH 8301 MmPmUYloemG2aX;uJGF{e2G7 Ml70NlAhyrWP M1O1cFEhcA>? NGjBW4xKdmO{ZXHz[ZMh[2WubDDtbYdz[XSrb36= NETzUlEyQTh7NkS3OS=>
Swiss3T3 NHmzbVZEd2yxbomt[o9zdWmwZzDBd5NigQ>? MlLBNVAhyrWP NXzBT|czOTNiZB?= MXzJcoNz\WG|ZYOgdJJwe3SjdHWgZ4VtdCClb3zvcpku\m:{bXnu[{Bi[3Srdnn0fS=> MX:yNVQ3PDlyMh?=
HT22 M4myRWN6fG:2b4jpZ{BCe3OjeR?= Mo\vNVAhyrWP M{HSOVE{KGh? NVvMVIN2WHKxdHXjeJMh[WejaX7zeEBodHW2YX3heIUucW6mdXPl[EBv\XW{b37hcEBl\WG2aB?= NUXJTI52OjJ6MUC4N|U>
Salivary gland stem cells NEPwepFHfW6ldHnvckBCe3OjeR?= MmDzNVAhyrWP NH3S[4g4KGR? NGD0WJFT\WS3Y3XzJHNIW0Nic3Xu[ZNk\W6lZR?= M3n2RVI2QDB2NU[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 to the product individually and in order(Data is from Selleck tests instead of citations):
saline
For best results, use promptly after mixing.
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

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