Y-27632 2HCl

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。

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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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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 NXu1WJN1TnWwY4Tpc44hSXO|YYm= MWGxNEDPxE1? NEHzdVAzKGh? NVHyb4g6TE2VTx?= NXP1boJUUW6qaXLpeJMhfGinIHHzd4Vu[my7IH;mJI1q[3KxdIXieYxmeyCjbnSgbY51\XKvZXTpZZRmKG[rbHHt[Y51eyC2bzDmc5JuKGW6dHXu[IVlKHC{b3Pld5Nmew>? NXfjSHFRQTZ2N{[1OC=>
N1E-115 NWG2WGYxTnWwY4Tpc44hSXO|YYm= MVGxNEDPxE1? MVqyJIg> NGjrO4JFVVOR Mn;wTY5pcWKrdIOgeIhmKGG|c3XtZox6KG:oIH3pZ5JwfHWkdXzld{BidmRiaX70[ZJu\WSrYYTlJIZqdGGvZX70d{B1dyCob4LtJIV5fGWwZHXkJJBzd2Onc4Pldy=> Mom1PVY1PzZ3NB?=
HeLa M4j1cGZ2dmO2aX;uJGF{e2G7 M3fqTFExKM7:TR?= MWOzNEBucW5? M2TuPGlvcGmkaYTzJJRp\SCob4LtZZRqd25ib3[gd5Rz\XO|IH\pZoVzeyCjbnSgeIhmKGG|c3XtZox6KG:oII\pcoN2dGmwLXPvcpRicW6rbneg[o9k[WxiYXTo[ZNqd26| NELWdYI6PjZ6MEey
CCL39 NIPwPZlHfW6ldHnvckBCe3OjeR?= M4i3bVMxKM7:TR?= MXezNEBucW5? NVLJT5pIS2:vcHzleIVtgSCjYn;sbZNp\XNiYXP0bZZifGmxbjDv[kBP[S2KIHX4Z4hidmencjDOTGUyKGK7IHnueIVoemmwcx?= MkL6PVY6OzN6Mh?=
Mesothelial cells from rat mesentery MkPTTY53[XOrdnWgRZN{[Xl? MmHCN|Ah|ryP MXmyNEBp M1vhdmJtd2OtczDpcpZie2m4ZTDhZ5Rqfmm2eR?= MlrXPVk{ODh5Mh?=
NIH3T3 MmrqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUCxNEDPxE1? NX2zRphjOThiZB?= NWTEboZZTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? NFPtZlAyODB{MUO4Oi=>
Dbl-d NUS4cpdmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGK0bHkyOCEQvF2= MkfRNVgh\A>? M2fhW3N1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp MoP2NVAxOjF|OE[=
Dbl-e MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH:3RWIyOCEQvF2= NGXrXosyQCCm MoLRUY9l\XKjdHXsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NWX5b3VOOTByMkGzPFY>
mNET1-d MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVexNEDPxE1? M1PyclE5KGR? NXL4TFFZW3S{b37ncJkhcW6qaXLpeJMh[2WubDDndo94fGh? MVyxNFAzOTN6Nh?=
mNET1-e MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\HWG5nOTBizszN MoPvNVgh\A>? MWXTeJJwdmeueTDpcohq[mm2czDj[YxtKGe{b4f0bC=> NGDl[3kyODB{MUO4Oi=>
Ras-2 M1\Lb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnL6NVAh|ryP MYixPEBl MYnTeJJwdmeueTDpcohq[mm2czDj[YxtKGe{b4f0bC=> NFPydXAyODB{MUO4Oi=>
Ras-4 NYDsWnBkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPVNVAh|ryP MX:xPEBl NEXHcWFUfHKxbnfsfUBqdmirYnn0d{Bk\WyuIHfyc5d1cA>? Ml32NVAxOjF|OE[=
Src-1 NWPyWW5kT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFe2R24yOCEQvF2= NILzfYkyQCCm MX;Ec4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To MUWxNFAzOTN6Nh?=
Src-4 MmHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVSxNEDPxE1? NUHwS5BCOThiZB?= NWHBcYluTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? NVjifXhoOTByMkGzPFY>
NIH3T3 NELMdGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjpT3htOTBizszN NFm0V5AyQCCm NGH2eVVFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp NUjNU4Y5OTByMkGzPFY>
Src-1 NEX4fIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFP1W4QyOCEQvF2= MonXNVgh\A>? NGTzU2NFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp MorTNVAxOjF|OE[=
Src-2 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfBRpcyOCEQvF2= MVqxPEBl NFzkTJlFd2W|IH7veEBqdmirYnn0JINmdGxiZ4Lve5Rp M3u3NVExODJzM{i2
SW620 M2DQXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWS5T3ZLOTBizszN NF3jTYgyQCCm MULEc4V{KG6xdDDpcohq[mm2IHPlcIwh\3Kxd4To NG\5[owyODB{MUO4Oi=>
HCT15 Ml\OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPSNZI{OTBizszN NXzDdpg4OThiZB?= NX;NPZVGTG:nczDuc5QhcW6qaXLpeEBk\WyuIHfyc5d1cA>? M2j0SlExODJzM{i2
HCT116 M323Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TlNVExKM7:TR?= NFO4[WgyQCCm M2LUOHN1em:wZ3z5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp MknmNVAxOjF|OE[=
LS174T MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXqxNEDPxE1? MVOxPEBl MYfNc4RmemG2ZXz5JIlvcGmkaYTzJINmdGxiZ4Lve5Rp NX73T2FUOTByMkGzPFY>
Neonatal rat ventricular myocytes NFr3dmZHfW6ldHnvckBCe3OjeR?= NHLzTmgyOCEQvF2= MXq0PEBp NGnSco9KdmirYnn0d{BGXC1zLXnu[JVk\WRiaX7jdoVie2W|IHnuJJBzd3SnaX6gd5lvfGinc3nzMEBk\WyuIIPpfoUh[W6mIH35c4Zq[nKrbHzhdkBwemejbnn6ZZRqd25? Mo\DNVA{QDZ4MUO=
Stellate Cell Ml\vSpVv[3Srb36gRZN{[Xl? MVqyOUDPxE1? NWHMVotQOTVibXnu NIe0U25KdmirYnn0d{Bnd3KvYYTpc44hd2ZiRj3hZ5RqdiC|dILld5Mh\mmkZYLzJIFv\CCyaH;zdIhwenmuYYTpc44hd2ZibYnvd4lvKGyrZ3j0JINp[Wmw MnXyNVA3ODB2OU[=
Rat Vascular Smooth Muscle Cells MVXGeY5kfGmxbjDBd5NigQ>? NYnTeHp1OTBizszN NXXpS2dUOiCq NFXDUm1KdmirYnn0d{Bidmerb4TlcpNqdiCLST3pcoR2[2WmIHj5dIVzfHKxcHj5 NYe4WmNQOTB4NEKzNVc>
PC3 MXnGeY5kfGmxbjDBd5NigQ>? NX\5S5JzOjVizszN MYKxJIg> MXXJcoR2[2W|IH3vdpBpd2yxZ3njZYwh[2ijbnfldy=> NILLb40yODd{MES3NS=>
PC3 M1PwcG1q\3KjdHnvckBCe3OjeR?= MmXYNlUh|ryP M2LDNlEhcA>? NXPFTpdFUW6qaXLpeJMhfGinIFLNSmIuS01iYX7kJJRp\SCHR1[td5RqdXWuYYTl[EBucWe{YYTpc44> MVyxNFczODR5MR?=
PC3 M3TG[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHWNlUh|ryP M3LW[|E4KGh? M2HaOWRw\XNibn;0JIlvcGmkaYSgZ4VtdCCpcn;3eIg> M{LTeFExPzJyNEex
LNCaP M1npOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWiyOUDPxE1? M2To[|E4KGh? MkH5SI9meyCwb4SgbY5pcWKrdDDj[YxtKGe{b4f0bC=> MXGxNFczODR5MR?=
Rat hepatic stellate cells MWHGeY5kfGmxbjDBd5NigQ>? NEftTJA{OCEQvF2= M2rX[VQ5KGh? M4exVmRqdWmwaYPo[ZMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDFdoszNCCjbnSg[IVkemWjc3XzJI5mfyCGTlGgd5lvfGinc3nz Mn36NVA5PDV4NkO=
Pancreatic acinar cells MoHVSpVv[3Srb36gRZN{[Xl? NYfG[VlMOTEEoN88US=> NUHvU5ZjPzBibXnu NEPEWGhRd3SnboTpZZRmeyCFQ1utd5RqdXWuYYTl[EBx[W6lcnXheIlkKGWweont[UB{\WO{ZYTpc44> M3rJOFEzPzR3MEiw
C2C12 NEH0[GJHfW6ldHnvckBCe3OjeR?= NWK2bGhvOTEEoN88US=> NWjnWlZVPiCq MlfqVJJmfmWwdIOgeIhmKHOncnnu[UBxcG:|cHjvdplt[XSrb36gc4YhUVKVLUGgbY5lfWOnZDDifUBqdnO3bHnuJIFv\C:xcjDUUmYu|rF? NV3rNpB6OTZ{NkexNlQ>
PC 12 NH3MfXVHfW6ldHnvckBCe3OjeR?= M4fBT|ExyqEQvF2= NFf0dGYzPCCq MXPBeJRmdnWjdHXzJINifGWlaH;sZY1qdmViYnnvd5lvfGinc3nz MXuxOlIyQTR{NB?=
Cynomolgus monkey embryonic stem cells MnzOR5l1d3SxeHnjJGF{e2G7 MljuNlAhyrWP MWiyOEBp NYn6RXlwWHKxbX;0[ZMh[3mHUzDj[YxtKHO3co\peoFt NGTnT3EyQDl2MEi1OS=>
TSGH 8301 MXvNbYdz[XSrb36gRZN{[Xl? NVH5bHgxOjBiwsXN MnnYNUBp NH3uTINKdmO{ZXHz[ZMh[2WubDDtbYdz[XSrb36= M2TrS|E6QDl4NEe1
Swiss3T3 MWLDc4xwdnlvZn;ycYlv\yCDc4PhfS=> NV;CSVEyOTBiwsXN NWjGdlZIOTNiZB?= MVLJcoNz\WG|ZYOgdJJwe3SjdHWgZ4VtdCClb3zvcpku\m:{bXnu[{Bi[3Srdnn0fS=> M1y1flIyPDZ2OUCy
HT22 NYjqWXBuS3m2b4TvfIlkKEG|c3H5 MmfaNVAhyrWP MmL5NVMhcA>? M4DIO3Bzd3SnY4TzJIFo[Wmwc4Sg[4x2fGGvYYTlMYlv\HWlZXSgcoV2em:wYXyg[IVifGh? NV7xSWRGOjJ6MUC4N|U>
Salivary gland stem cells M1PDWWZ2dmO2aX;uJGF{e2G7 NH7YeHUyOCEEtV2= MorSO{Bl NFjodlhT\WS3Y3XzJHNIW0Nic3Xu[ZNk\W6lZR?= MWqyOVgxPDV4MB?=

... 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]
+ 展开
  • 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
  • Formulation: 溶于DMSO,然后在盐水中稀释 (大鼠); 0.9% NaCl (小鼠)
  • 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
稳定性 powder
in solvent
别名 N/A

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 (g) = 浓度 (mol/L) x 体积 (L) 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

技术支持

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID