Y-27632 2HCl

For research use only. Not for use in humans.

目录号:S1049

Y-27632 2HCl Chemical Structure

Molecular Weight(MW): 320.26

Y-27632 2HCl是一种选择性ROCK1(p160ROCK)抑制剂,无细胞试验中Ki为140 nM,比对其他激酶包括PKC,cAMP依赖性蛋白激酶,MLCK和PAK的作用强200多倍。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1278.83 现货
RMB 576.16 现货
RMB 972.96 现货
RMB 1396.58 现货
RMB 4674.45 现货
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客户使用Selleck生产的Y-27632 2HCl发表文献397篇:

产品安全说明书

ROCK抑制剂选择性比较

生物活性

产品描述 Y-27632 2HCl是一种选择性ROCK1(p160ROCK)抑制剂,无细胞试验中Ki为140 nM,比对其他激酶包括PKC,cAMP依赖性蛋白激酶,MLCK和PAK的作用强200多倍。
靶点
ROCK1 (p160ROCK) [1]
(Cell-free assay)
ROCK2 [6]
(Cell-free assay)
140 nM(Ki) 300 nM(Ki)
体外研究

Y-27632也同等有效抑制ROCK-II。Y-27632作用于PKC, cAMP依赖的蛋白激酶和 肌球蛋白轻链激酶(MLCK)几乎没有活性,Ki分别为26 μM, 25 μM, 和 > 250 μM。Y-27632通过选择性抑制Ca2+敏感化,而抑制多种兴奋剂而不是KCl,包括Phenylephrine, Histamine, Acetylcholine, Serotonin, Endothelin,和Thromboxane诱导的平滑肌收缩,IC50为0.3-1 μM。Y-27632 作用于培养的细胞,抑制Rho诱导的, p160ROCK调节的应力纤维的形成。[1] Y-27632处理,阻断 Rho调节的肌动球蛋白的激活,也阻断LPA刺激的MM1 细胞入侵活性,这种作用存在浓度依赖性。[2] 10 μM Y-27632 处理在无血清悬浮(SFEB)培养基中的人类胚胎干细胞(hES),显著减少分离诱导的凋亡,提高克隆效率(从~1%提高到~27%), 转基因后促进亚克隆,且使SFEB培养的hES细胞存活及分化成Bf1+皮质和基底端脑祖细胞。[5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Swiss 3T3 cells M{nQVWZ2dmO2aX;uJGF{e2G7 NEn0e4IyOCEQvF2= NImyXJIzKGh? M{\QXWROW09? NGTEc|hKdmirYnn0d{B1cGViYYPz[Y1jdHlib3[gcYlkem:2dXL1cIV{KGGwZDDpcpRmem2nZHnheIUh\mmuYX3lcpR{KHSxIH\vdo0h\Xi2ZX7k[YQheHKxY3Xzd4V{ MXu5OlQ4PjV2
N1E-115 MmrjSpVv[3Srb36gRZN{[Xl? NVzheJNyOTBizszN NF\IWVQzKGh? MXrEUXNQ Mk\nTY5pcWKrdIOgeIhmKGG|c3XtZox6KG:oIH3pZ5JwfHWkdXzld{BidmRiaX70[ZJu\WSrYYTlJIZqdGGvZX70d{B1dyCob4LtJIV5fGWwZHXkJJBzd2Onc4Pldy=> NV7yZmJxQTZ2N{[1OC=>
HeLa NHLsTo5HfW6ldHnvckBCe3OjeR?= MkP6NVAh|ryP NWW4[plwOzBibXnu M{XifGlvcGmkaYTzJJRp\SCob4LtZZRqd25ib3[gd5Rz\XO|IH\pZoVzeyCjbnSgeIhmKGG|c3XtZox6KG:oII\pcoN2dGmwLXPvcpRicW6rbneg[o9k[WxiYXTo[ZNqd26| NVS3ZVNVQTZ4OEC3Ni=>
CCL39 NXnGXXJ7TnWwY4Tpc44hSXO|YYm= MV6zNEDPxE1? MVqzNEBucW5? NXr6VI04S2:vcHzleIVtgSCjYn;sbZNp\XNiYXP0bZZifGmxbjDv[kBP[S2KIHX4Z4hidmencjDOTGUyKGK7IHnueIVoemmwcx?= NE\tfWM6Pjl|M{iy
Mesothelial cells from rat mesentery NYfu[llLUW64YYPpeoUhSXO|YYm= NHPCO5U{OCEQvF2= NV\5OmhQOjBiaB?= MUDCcI9kc3NiaX72ZZNqfmViYXP0bZZqfHl? MYS5PVMxQDd{
NIH3T3 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fXbFExKM7:TR?= M4TJO|E5KGR? MVPEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To MoLTNVAxOjF|OE[=
Dbl-d MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXjRpYyOCEQvF2= MYqxPEBl MmPlV5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MVGxNFAzOTN6Nh?=
Dbl-e MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3lNVAh|ryP MYqxPEBl NXqybmt4VW:mZYLheIVtgSCrbnjpZol1eyClZXzsJIdzd3e2aB?= NVvkVGJyOTByMkGzPFY>
mNET1-d M4P0SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPXNVAh|ryP M4P3T|E5KGR? MmjKV5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NY[3W2JYOTByMkGzPFY>
mNET1-e NYTlU2dNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPqVXcyOCEQvF2= M{D0c|E5KGR? NHPDV5RUfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NFrBRnIyODB{MUO4Oi=>
Ras-2 NHPaTI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjZV|MyOCEQvF2= MnX0NVgh\A>? MXnTeJJwdmeueTDpcohq[mm2czDj[YxtKGe{b4f0bC=> MYqxNFAzOTN6Nh?=
Ras-4 NUO1OYpCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXW2XnQ3OTBizszN MXqxPEBl NFPwZmNUfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NI\kV4cyODB{MUO4Oi=>
Src-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fN[VExKM7:TR?= NXniOmRROThiZB?= MYjEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To MmjNNVAxOjF|OE[=
Src-4 NX7tNpZpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVOxNEDPxE1? M{nUc|E5KGR? NW[2OHNoTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? NYL0ZYd7OTByMkGzPFY>
NIH3T3 MonNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjlNVAh|ryP M{foVlE5KGR? NUS3enRWTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? M4PuPVExODJzM{i2
Src-1 MnPnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETCc5YyOCEQvF2= M1\OXlE5KGR? MkjESI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> MkHWNVAxOjF|OE[=
Src-2 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rjXFExKM7:TR?= NHqzZo0yQCCm Ml3DSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> MYGxNFAzOTN6Nh?=
SW620 NELWb3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XIXVExKM7:TR?= MWCxPEBl MXLEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To M2Htc|ExODJzM{i2
HCT15 MmnsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M376VFExKM7:TR?= M4PBe|E5KGR? MnLaSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> NVrGPI1nOTByMkGzPFY>
HCT116 Mn7YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDhb5UyOCEQvF2= NWO3[XpxOThiZB?= NIjkOIJUfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? M3eyVFExODJzM{i2
LS174T MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3zVFUyOCEQvF2= NFPUVpoyQCCm NFTGNnhOd2SncnH0[Yx6KGmwaHnibZR{KGOnbHyg[5Jwf3Sq NYLIbGI2OTByMkGzPFY>
Neonatal rat ventricular myocytes M4\mZWZ2dmO2aX;uJGF{e2G7 M4LIZVExKM7:TR?= MlPrOFghcA>? M4HxbWlvcGmkaYTzJGVVNTFvaX7keYNm\CCrbnPy[YF{\XNiaX6gdJJwfGWrbjDzfY51cGW|aYOsJINmdGxic3n6[UBidmRibYnv[oljemmubHHyJI9z\2GwaYrheIlwdg>? MkXuNVA{QDZ4MUO=
Stellate Cell MWXGeY5kfGmxbjDBd5NigQ>? MYmyOUDPxE1? NXSw[5RWOTVibXnu NGTLPYJKdmirYnn0d{Bnd3KvYYTpc44hd2ZiRj3hZ5RqdiC|dILld5Mh\mmkZYLzJIFv\CCyaH;zdIhwenmuYYTpc44hd2ZibYnvd4lvKGyrZ3j0JINp[Wmw NES5Z3gyODZyMES5Oi=>
Rat Vascular Smooth Muscle Cells NFrGTHVHfW6ldHnvckBCe3OjeR?= M{LrRlExKM7:TR?= M4H6b|IhcA>? MVTJcohq[mm2czDhcodqd3SnboPpckBKUS2rbnT1Z4VlKGi7cHXyeJJweGi7 NFfYcXEyODZ2MkOxOy=>
PC3 NXj5SlRITnWwY4Tpc44hSXO|YYm= NFPLbmIzPSEQvF2= MYmxJIg> NH:wS3FKdmS3Y3XzJI1wenCqb3zv[4lk[WxiY3jhcodmew>? MUixNFczODR5MR?=
PC3 M{DuTG1q\3KjdHnvckBCe3OjeR?= NFXtRVczPSEQvF2= NHTTU5UyKGh? MmPETY5pcWKrdIOgeIhmKEKPRlKtR20h[W6mIITo[UBGT0Zvc4TpcZVt[XSnZDDtbYdz[XSrb36= MXuxNFczODR5MR?=
PC3 Ml\iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzWNlUh|ryP MXSxO{Bp NXfy[WdTTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? NELrbZIyODd{MES3NS=>
LNCaP M3jVSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWWyOUDPxE1? M3rOOlE4KGh? NGTOcm5Fd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp NEG4PYIyODd{MES3NS=>
Rat hepatic stellate cells NGHDO5ZHfW6ldHnvckBCe3OjeR?= NYrPeZRWOzBizszN M{XxTVQ5KGh? NX;LU3RQTGmvaX7pd4hmeyC2aHWgdIhwe3Cqb4L5cIF1cW:wIH;mJGVzczJuIHHu[EBl\WO{ZXHz[ZMhdmW5IFTORUB{gW62aHXzbZM> NGrlU|QyODh2NU[2Ny=>
Pancreatic acinar cells Mk[zSpVv[3Srb36gRZN{[Xl? NFH4VGsyOMLizszN MYe3NEBucW5? M3XtNXBwfGWwdHnheIV{KEOFSz3zeIlufWyjdHXkJJBidmO{ZXH0bYMh\W68eX3lJJNm[3KndHnvci=> NWXhfJpZOTJ5NEWwPFA>
C2C12 MlXSSpVv[3Srb36gRZN{[Xl? NVy2VVJ2OTEEoN88US=> M1zuTVYhcA>? NYO4e3h4WHKndnXueJMhfGinIIPldolv\SCyaH;zdIhwenmuYYTpc44hd2ZiSWLTMVEhcW6mdXPl[EBjgSCrboP1cIlvKGGwZD;vdkBVVkZvzsG= NVnyeG51OTZ{NkexNlQ>
PC 12 NFu4VlNHfW6ldHnvckBCe3OjeR?= MXqxNOKh|ryP NVz2SYlrOjRiaB?= NG\VV4xCfHSnboXheIV{KGOjdHXjbI9t[W2rbnWgZolwe3mwdHjld4l{ M3f1N|E3OjF7NEK0
Cynomolgus monkey embryonic stem cells MmLJR5l1d3SxeHnjJGF{e2G7 M{nifFIxKML3TR?= M1;ufFI1KGh? M{XoOHBzd22xdHXzJIN6TVNiY3XscEB{fXK4aY\hcC=> MoXiNVg6PDB6NUW=
TSGH 8301 NGXYbodOcWe{YYTpc44hSXO|YYm= NEC0XlkzOCEEtV2= MYKxJIg> M{nIfGlv[3KnYYPld{Bk\WyuIH3p[5JifGmxbh?= MlzWNVk5QTZ2N{W=
Swiss3T3 NYr4WVBiS2:ub375MYZwem2rbnegRZN{[Xl? MV[xNEDDvU1? NVLDeHBPOTNiZB?= NV7zTIFCUW6lcnXhd4V{KHC{b4P0ZZRmKGOnbHygZ49td267LX\vdo1qdmdiYXP0bZZqfHl? MWiyNVQ3PDlyMh?=
HT22 NIfxNYlEgXSxdH;4bYMhSXO|YYm= NXjNVXpFOTBiwsXN NVnWN|lXOTNiaB?= NITrTmRRem:2ZXP0d{Bi\2GrboP0JIdtfXSjbXH0[U1qdmS3Y3XkJI5mfXKxbnHsJIRm[XSq M{LJZlIzQDFyOEO1
Salivary gland stem cells NWn3eFhHTnWwY4Tpc44hSXO|YYm= M3nrXlExKML3TR?= NG\tUJc4KGR? MnrVVoVlfWOnczDTS3NEKHOnbnXzZ4Vv[2V? M37odVI2QDB2NU[w

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western Blot
p-LIMK1(Thr508); 

PubMed: 24704720     


Immunoblot analysis of HCT116 and HCT116 SMAD4-/- cells. Cells were transfected transiently with either BMPR2 or pcDNA vector. Subsequently, cells were treated with 2.5 μmol/L of ROCK inhibitor (Y-27632) or PBS. Blots were incubated with antibodies against pLIMK1/2 and p-cofilin. Actin was used as a loading control.

p-LIMK2(Thr505); 

PubMed: 24704720     


Immunoblot analysis of HCT116 and HCT116 SMAD4-/- cells. Cells were transfected transiently with either BMPR2 or pcDNA vector. Subsequently, cells were treated with 2.5 μmol/L of ROCK inhibitor (Y-27632) or PBS. Blots were incubated with antibodies against pLIMK1/2 and p-cofilin. Actin was used as a loading control.

p-Cofilin(Ser3); 

PubMed: 24704720     


Immunoblot analysis of HCT116 and HCT116 SMAD4-/- cells. Cells were transfected transiently with either BMPR2 or pcDNA vector. Subsequently, cells were treated with 2.5 μmol/L of ROCK inhibitor (Y-27632) or PBS. Blots were incubated with antibodies against pLIMK1/2 and p-cofilin. Actin was used as a loading control.

CDK2; 

PubMed: 26555939     


Western blot detected proteins changes pTR cells cultured with Y-27632. CDX2 was remarkably increased in Y-27632 treated pIVFTR-7 and pPATR-5 cells. pTR cells cultured without Y-27632 in the same condition are used as control. β-ACTIN serves as an endogenous control. 

KRT7; 

PubMed: 26555939     


Western blot detected proteins changes pTR cells cultured with Y-27632. CDX2 was remarkably increased in Y-27632 treated pIVFTR-7 and pPATR-5 cells. pTR cells cultured without Y-27632 in the same condition are used as control. β-ACTIN serves as an endogenous control. 

ROCK2; 

PubMed: 26555939     


Western blot detected proteins changes pTR cells cultured with Y-27632. CDX2 was remarkably increased in Y-27632 treated pIVFTR-7 and pPATR-5 cells. pTR cells cultured without Y-27632 in the same condition are used as control. β-ACTIN serves as an endogenous control. 

E-cadherin; 

PubMed: 27399334     


The expression and/or phosphorylation of E-cadherin and ROCKs downstream targets in SW-480-FOXM1D cells treated with Y-27632.

p-MLC2(Ser19); 

PubMed: 27399334     


The expression and/or phosphorylation of E-cadherin and ROCKs downstream targets in SW-480-FOXM1D cells treated with Y-27632.

24704720 26555939 27399334
Transwell migration assay
cell migration inhibition ; 

PubMed: 27694793     


Data represent mean ± SEM, n=3. Compared with control, * P<0.05, ** P<0.01. Compared with control, Y-27632, or EGCG, *** P<0.01.

27694793
Immunofluorescence
Neurotoxicity Assay; 

PubMed: 21362567     


Representations of neurodegeneration in H9-, HUF5- and G2019S-iPSC derived neurons when treated with neurotoxins, H2O2 and MG-132, and ROCK inhibitor Y-27632. Scale bar = 50 µm.

E-cadherin; 

PubMed: 24523903     


The localized patterns of E-cadherin and b-catenin were examined using specific antibodies through confocal laser microscopy. MCF-7 cells were cultured for 24 hrs in the absence or presence of Y-27632 (20 µM) to inhibit ROCK activity. 

beta-catenin; 

PubMed: 24523903     


The localized patterns of E-cadherin and b-catenin were examined using specific antibodies through confocal laser microscopy. MCF-7 cells were cultured for 24 hrs in the absence or presence of Y-27632 (20 µM) to inhibit ROCK activity. 

Phalloidin; 

PubMed: 27399334     


Triple IF staining for F-actin (phalloidin, green) E-cadherin (b) (red) and nuclei (DAPI, blue) showed decreased F-actin, increased E-cadherin and altered cell shape and size in SW-480-FOXM1D cells treated with the ROCKs inhibitor Y-27632 or fasudil (both 10 μM, for 24 h). Scale bar, 25 μm. 

21362567 24523903 27399334
Growth inhibition assay
cell proliferation ; 

PubMed: 24523903     


MCF-7 cells and MDA-MB-231 cells were cultured on tissue culture plates for four days with or without Y-27632 (20 µM). Relative cell proliferation rates were determined by the cell number assayed using CCK-8 kit. The data are expressed as the mean ± SD. n = 3 culture dishes. The p-value was less than 0.05 for comparisons between control (Control) and treatment groups (Y-27632) in MCF-7 cells. *, p<0.05.

24523903
ELISA
caspase-9; 

PubMed: 30320378     


Caspase-9 activity was measured via ELISA. Mst1-mediated casapse-9 activation was inhibited by Y-27632 in A549 cells. *P<0.05. Ad, adenovirus; Mst1, mammalian STE20-like kinase 1.

30320378
体内研究 Y-27632按30 mg/kg剂量口服处理自发性高血压大鼠,肾性高血压大鼠,及去氧皮质酮醋酸(DOCA)盐高血压大鼠,显著降低血压,这种作用存在剂量依赖性。[1]Y-27632按每小时0.55 μL通过植入泵持续处理表达Val14-RhoA的大鼠,持续11天,延迟 MM1 细胞入侵。[2] Y-27632作用于肺循环,通过抑制ROCK, 降低 缺氧诱导的血管生成,和血管重构。[4]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

动物实验:[1] [7]
- 合并
  • Animal Models: 携带自发或诱发高血压的雄性Wistar大鼠; 艾利希腹水癌小鼠模型
  • Dosages: 30 mg/kg/day (大鼠);0-10 mg/kg (小鼠)
  • Administration: 口服处理 (大鼠);ip(小鼠)
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 64 mg/mL warmed (199.83 mM)
Water 14 mg/mL (43.71 mM)
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
saline
10mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 320.26
化学式

C14H21N3O.2HCl

CAS号 129830-38-2
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

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操作手册

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常见问题及建议解决方法

  • 问题 1:

    Is there any data about the Amax (maximum attraction luminosity) and extinction coefficient of this compound?

  • 回答:

    The wavelength we used to test HPLC is 260nm while the extinction coefficient is unknown.

  • 问题 2:

    Could this product be used in cell culture? Do you have any reference for this application?

  • 回答:

    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.

ROCK Signaling Pathway Map

ROCK Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID