Y-27632 2HCl

For research use only. Not for use in humans.

目录号：S1049

Y-27632 2HCl Chemical Structure

CAS No. 129830-38-2

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531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 M4n5d2Z2dmO2aX;uJGF{e2G7 MkW4NVAh|ryP MkTaNkBp NGrpUFRFVVOR NYjjbVBTUW6qaXLpeJMhfGinIHHzd4Vu[my7IH;mJI1q[3KxdIXieYxmeyCjbnSgbY51\XKvZXTpZZRmKG[rbHHt[Y51eyC2bzDmc5JuKGW6dHXu[IVlKHC{b3Pld5Nmew>? NITRdFY6PjR5NkW0
N1E-115 M2DUUWZ2dmO2aX;uJGF{e2G7 M{HJclExKM7:TR?= NE\COlQzKGh? NWTjZoN2TE2VTx?= NWm2bJU4UW6qaXLpeJMhfGinIHHzd4Vu[my7IH;mJI1q[3KxdIXieYxmeyCjbnSgbY51\XKvZXTpZZRmKG[rbHHt[Y51eyC2bzDmc5JuKGW6dHXu[IVlKHC{b3Pld5Nmew>? MojZPVY1PzZ3NB?=
HeLa NXX4PFVbTnWwY4Tpc44hSXO|YYm= MX2xNEDPxE1? MnXMN|AhdWmw NF;pVllKdmirYnn0d{B1cGViZn;ycYF1cW:wIH;mJJN1emW|czDmbYJmenNiYX7kJJRp\SCjc4PlcYJtgSCxZjD2bY5kfWyrbj3jc451[WmwaX7nJIZw[2GuIHHkbIV{cW:wcx?= MYm5OlY5ODd{
CCL39 M362Z2Z2dmO2aX;uJGF{e2G7 MlfPN|Ah|ryP M1no[|MxKG2rbh?= MVjDc41xdGW2ZXz5JIFjd2yrc3jld{Bi[3SrdnH0bY9vKG:oIF7hMWgh\XilaHHu[4VzKE6KRUGgZpkhcW62ZXfybY5{ NIH3b3U6Pjl|M{iy
Mesothelial cells from rat mesentery M3LOdGlvfmG|aY\lJGF{e2G7 NXnjVVMxOzBizszN MmXONlAhcA>? M1rFcGJtd2OtczDpcpZie2m4ZTDhZ5Rqfmm2eR?= NEnOS5M6QTNyOEey
NIH3T3 NXjOXWJ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\Fb|ExKM7:TR?= NY\ZOXVHOThiZB?= MYDEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To NXf2ZWd4OTByMkGzPFY>
Dbl-d MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\3dXEyOCEQvF2= NF\kcpAyQCCm MV7TeJJwdmeueTDpcohq[mm2czDj[YxtKGe{b4f0bC=> MUexNFAzOTN6Nh?=
Dbl-e NIfnfHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TXUVExKM7:TR?= NED5b|UyQCCm MWfNc4RmemG2ZXz5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp M3XCXVExODJzM{i2
mNET1-d NYrHW2diT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;0XWwyOTBizszN NYP4[GNbOThiZB?= NHXFPGhUfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NWj6RWpROTByMkGzPFY>
mNET1-e MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3S4TFExKM7:TR?= MoPTNVgh\A>? NHXqO|BUfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NEDTeJIyODB{MUO4Oi=>
Ras-2 NHzheXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33zZVExKM7:TR?= NHfrcGcyQCCm MUTTeJJwdmeueTDpcohq[mm2czDj[YxtKGe{b4f0bC=> NGLQWHcyODB{MUO4Oi=>
Ras-4 M37pNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnwPJgyOCEQvF2= MXSxPEBl MlXEV5Rzd26pbImgbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NHq1[4EyODB{MUO4Oi=>
Src-1 NHHTc4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnaNVAh|ryP Mn\lNVgh\A>? M{exNGRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> M2DKPFExODJzM{i2
Src-4 M3rFPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLqNVAh|ryP MWKxPEBl MUnEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To NF24[4cyODB{MUO4Oi=>
NIH3T3 NXmySlFIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmryNVAh|ryP MYmxPEBl Mn7hSI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> Mof2NVAxOjF|OE[=
Src-1 MkfBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jMflExKM7:TR?= NGrablMyQCCm NYj4eY1STG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? NGHMclgyODB{MUO4Oi=>
Src-2 M{TyNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPNN3gyOCEQvF2= M3HsUlE5KGR? NX7ZblVXTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? M1HhT|ExODJzM{i2
SW620 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvXNVAh|ryP NYS1N3V5OThiZB?= NHLBU2xFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp MoXlNVAxOjF|OE[=
HCT15 NYnV[mxXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInTPGwyOCEQvF2= MU[xPEBl MkT4SI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> MmjINVAxOjF|OE[=
HCT116 NGr4em5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXuxNEDPxE1? NYi0UoFsOThiZB?= M2rZcXN1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp MYqxNFAzOTN6Nh?=
LS174T MmLPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGf2XnMyOCEQvF2= M2nzWVE5KGR? NGLkcVROd2SncnH0[Yx6KGmwaHnibZR{KGOnbHyg[5Jwf3Sq NGewNWwyODB{MUO4Oi=>
Neonatal rat ventricular myocytes M1flcmZ2dmO2aX;uJGF{e2G7 MXOxNEDPxE1? MUO0PEBp MYfJcohq[mm2czDFWE0yNWmwZIXj[YQhcW6lcnXhd4V{KGmwIIDyc5RmcW5ic4nueIhme2m|LDDj[YxtKHOrenWgZY5lKG27b3\pZpJqdGyjcjDvdodidmm8YYTpc44> MmjNNVA{QDZ4MUO=
Stellate Cell MXrGeY5kfGmxbjDBd5NigQ>? NGXScVAzPSEQvF2= MkT1NVUhdWmw M{W3fGlvcGmkaYTzJIZwem2jdHnvckBw\iCILXHjeIlvKHO2cnXzd{BncWKncoOgZY5lKHCqb4PwbI9zgWyjdHnvckBw\iCveX;zbY4hdGmpaISgZ4hicW5? Mm\4NVA3ODB2OU[=
Rat Vascular Smooth Muscle Cells NUfDfFhrTnWwY4Tpc44hSXO|YYm= M2PCNlExKM7:TR?= M37oblIhcA>? MWPJcohq[mm2czDhcodqd3SnboPpckBKUS2rbnT1Z4VlKGi7cHXyeJJweGi7 NXfD[5lOOTB4NEKzNVc>
PC3 M4TUZWZ2dmO2aX;uJGF{e2G7 NFL1WGMzPSEQvF2= NWDsOnAxOSCq MVTJcoR2[2W|IH3vdpBpd2yxZ3njZYwh[2ijbnfldy=> Mn64NVA4OjB2N{G=
PC3 MWPNbYdz[XSrb36gRZN{[Xl? NFnRU2QzPSEQvF2= MYKxJIg> NH;OXHRKdmirYnn0d{B1cGViQl3GRk1EVSCjbnSgeIhmKEWJRj3zeIlufWyjdHXkJI1q\3KjdHnvci=> MmPJNVA4OjB2N{G=
PC3 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVeyOUDPxE1? MmjSNVchcA>? NUX2b5JqTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? MlPhNVA4OjB2N{G=
LNCaP MnHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXUTm8zPSEQvF2= MWexO{Bp Moq5SI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> NHvz[ncyODd{MES3NS=>
Rat hepatic stellate cells NFPCUJpHfW6ldHnvckBCe3OjeR?= MlvWN|Ah|ryP NF7R[lQ1QCCq MlnpSIlucW6rc3jld{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFXyb|ItKGGwZDDk[YNz\WG|ZYOgcoV4KESQQTDzfY51cGW|aYO= NYDYUGV3OTB6NEW2OlM>
Pancreatic acinar cells MV\GeY5kfGmxbjDBd5NigQ>? NVzF[IF6OTEEoN88US=> NV;pfHNJPzBibXnu MnvpVI91\W62aXH0[ZMhS0ONLYP0bY12dGG2ZXSgdIFv[3KnYYTpZ{Bmdnq7bXWgd4VkemW2aX;u MUWxNlc1PTB6MB?=
C2C12 M3TvNGZ2dmO2aX;uJGF{e2G7 NUHMOJB2OTEEoN88US=> M1TFc|YhcA>? NIDTcVZRemW4ZX70d{B1cGVic3XybY5mKHCqb4PwbI9zgWyjdHnvckBw\iCLUmOtNUBqdmS3Y3XkJIJ6KGmwc4XsbY4h[W6mL3;yJHRPTi4QsR?= M1jFUFE3OjZ5MUK0
PC 12 NWnmOGM5TnWwY4Tpc44hSXO|YYm= M{frSVExyqEQvF2= NGn5c5czPCCq NFnuO2hCfHSnboXheIV{KGOjdHXjbI9t[W2rbnWgZolwe3mwdHjld4l{ M3vsZ|E3OjF7NEK0
Cynomolgus monkey embryonic stem cells MYnDfZRwfG:6aXOgRZN{[Xl? MnvRNlAhyrWP M1qwc|I1KGh? M2GwXnBzd22xdHXzJIN6TVNiY3XscEB{fXK4aY\hcC=> Ml7rNVg6PDB6NUW=
TSGH 8301 M{LNUG1q\3KjdHnvckBCe3OjeR?= M4XrdVIxKML3TR?= NV[4WYFpOSCq MlzBTY5kemWjc3XzJINmdGxibXnndoF1cW:w MYmxPVg6PjR5NR?=
Swiss3T3 MYPDc4xwdnlvZn;ycYlv\yCDc4PhfS=> Ml7sNVAhyrWP M13kNFE{KGR? Mn;GTY5kemWjc3XzJJBzd3O2YYTlJINmdGxiY3;sc456NW[xcn3pcoch[WO2aY\peJk> M1fYV|IyPDZ2OUCy
HT22 M4LK[mN6fG:2b4jpZ{BCe3OjeR?= Mlz4NVAhyrWP Ml[5NVMhcA>? Ml\OVJJwfGWldIOgZYdicW6|dDDncJV1[W2jdHWtbY5lfWOnZDDu[ZVzd26jbDDk[YF1cA>? MVSyNlgyODh|NR?=
Salivary gland stem cells NGfsdpVHfW6ldHnvckBCe3OjeR?= MnS0NVAhyrWP Mlv1O{Bl M2Pw[HJm\HWlZYOgV2dUSyC|ZX7ld4NmdmOn NHjo[IozPThyNEW2NC=>

... 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 只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；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

如果有其他问题，请给我们留言。

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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.

Selleck产品目录册

ROCK Signaling Pathway Map

ROCK Inhibitors with Unique Features

  • 选择性强的Rock抑制剂

    Fasudil (HA-1077) HCl : ROCK-II-selective, Ki=0.33 μM.

  • 活性最高的ROCK抑制剂

    GSK429286A : ROCK1, IC50=14 nM; ROCK2, IC50=63 nM.

  • 用于临床的ROCK抑制剂

    Fasudil (HA-1077) HCl : Phase III for scleroderma.

  • 最新的ROCK抑制剂

    RKI-1447 : Highly potent inhibitor of ROCK1 and ROCK2, with IC50 of 14.5 nM and 6.2 nM, respectively.

相关ROCK产品

  • Ro-3306 New

    RO-3306是一种ATP竞争性的选择性 CDK1 抑制剂，Ki 为20 nM，选择性是其他各种人类激酶的15倍多。RO-3306可增强p53介导的 Bax 激活和线粒体的凋亡。

  • CCG-1423 New

    CCG-1423是一种特定的 RhoA 通路抑制剂，能够抑制SRF介导的转录。

  • ML141 New

    ML141 (CID-2950007) 是 Rho 家族GTPase cdc42的一种有效的，选择性可逆非竞争性抑制剂，IC50为200 nM。对cdc42比对其他Rho家族中的GTPases(如Rac1, Rab2, Rab7)更有选择性。 ML141 与 p38 激活增加有关，并可能诱导p38依赖性凋亡/衰老。ML141还可保护神经母细胞瘤细胞免受二甲双胍(metformin)诱导的凋亡。

  • Thiazovivin

    Thiazovivin是一种新型ROCK抑制剂，无细胞试验中IC50为0.5 μM，在单细胞分离后，促进人胚胎干细胞（hESC）的存活。

  • GSK429286A

    GSK429286A (RHO-15)是一种选择性的ROCK1和ROCK2抑制剂，IC50分别为14 nM和63 nM。

    Features:More selective than Y-27632.

  • Fasudil (HA-1077) HCl

    Fasudil(HA-1077)是一种有效的、具有选择性的Rho抑制剂（ROCK2, Ki=0.33 μM），同时对PKA、PKG、PKC和MLCK也具有抑制活性，Ki值分别为1.6 μM、1.6 μM、3.3 μM、36 μM。Fasudil 也是calcium channel的阻滞剂。

  • RKI-1447

    RKI-1447是一种有效的ROCK1和ROCK2抑制剂，IC50分别为14.5 nM和6.2 nM，有抗侵入和抗肿瘤活性。

  • Palbociclib (PD-0332991) HCl

    Palbociclib (PD-0332991) HCl是一种高度选择性的CDK4/6抑制剂，无细胞试验中IC50分别为11 nM/16 nM。它对CDK1/2/5，EGFR，FGFR，PDGFR，InsR等没有抑制活性。Phase 3。

    Features:PD-0332991作为有应用前景的工具测定CDK激酶是否具有明显的治疗价值。

  • Alisertib (MLN8237)

    Alisertib (MLN8237)是一种选择性Aurora A抑制剂，无细胞试验中IC50为1.2 nM，作用于Aurora A比作用于Aurora B选择性强200倍以上。Alisertib 可诱导细胞周期阻滞、细胞凋亡与自噬。Phase 3。

    Features:MLN8237 是第一个口服有效的小分子Aurora A激酶选择性抑制剂。

  • Adavosertib (MK-1775)

    Adavosertib (MK-1775, AZD1775)是一种有效的，高选择性Wee1抑制剂，无细胞试验中IC50为5.2 nM；阻碍G2期DNA损伤检验点。Phase 2。

    Features:First reported Wee1 inhibitor

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID