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Y-27632 2HCl

Y-27632 2HCl是一種選擇性ROCK1和ROCK2抑制劑,無(wú)細(xì)胞試驗(yàn)中Ki分別為140 nM和300nM,比對(duì)其他激酶包括PKC,cAMP依賴性蛋白激酶,MLCK和PAK的作用強(qiáng)200多倍。

Y-27632 2HCl Chemical Structure

Y-27632 2HCl Chemical Structure

CAS: 129830-38-2

規(guī)格 價(jià)格 庫(kù)存 購(gòu)買數(shù)量
10mM (1mL in DMSO) 1278.83 現(xiàn)貨
2mg 576.16 現(xiàn)貨
5mg 972.96 現(xiàn)貨
10mg 1396.58 現(xiàn)貨
50mg 4674.45 現(xiàn)貨
200mg 7944.3 現(xiàn)貨
1g 16134.3 現(xiàn)貨
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常與Y-27632 2HCl一起在實(shí)驗(yàn)中被使用的化合物

SB202190


Y-27632 2HCl和SB202190,與其他抑制劑一起,使人原代真皮成纖維細(xì)胞中生成誘導(dǎo)性間充質(zhì)干細(xì)胞(iMSCs)。


Lai PL, et al. Sci Rep. 2017 Mar 17;7:44534.

SB431542


Y-27632 2HCl和SB431542聯(lián)合可逆轉(zhuǎn)mTEC-KO小鼠細(xì)胞中TGF-β1誘導(dǎo)的間充質(zhì)肌動(dòng)蛋白細(xì)胞骨架應(yīng)激纖維。


Das S, et al. BMC Cell Biol. 2009 Dec 21;10:94.

Laduviglusib (CHIR-99021)


Y-27632 2HCl和CHIR99021共同降低野生型(WT)和PKP2mut心肌細(xì)胞中脂肪生成基因的表達(dá)。


Parrotta EI, et al. Int J Mol Sci. 2021 Feb 18;22(4):2004.

MG132


Y-27632 2HCl可減少M(fèi)G132預(yù)處理后MYLA細(xì)胞中由TNFα引起的P-IκBα多聚泛素化。


Gallardo F, et al. Leukemia. 2018 Oct;32(10):2211-2223.

Z-VAD-FMK


Y27632 2HCl和Z-VAD-FMK可阻斷H2O2誘導(dǎo)的PC12細(xì)胞膜起泡和胞核凝聚。


Wang Y, et al. Front Mol Neurosci. 2017 Mar 14;10:75.

Y-27632 2HCl相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)信息
SW620 Growth Inhibition Assay 10 μM 18 d Does not inhibit cell growth 10021386
HCT15 Growth Inhibition Assay 10 μM 18 d Does not inhibit cell growth 10021386
HCT116 Growth Inhibition Assay 10 μM 18 d Strongly inhibits cell growth 10021386
LS174T Growth Inhibition Assay 10 μM 18 d Moderately inhibits cell growth 10021386
Neonatal rat ventricular myocytes Function Assay 10 μM 48 h Inhibits ET-1-induced increases in protein synthesis, cell size and myofibrillar organization 10386613
Stellate Cell Function Assay 25 μM 15 min Inhibits formation of F-actin stress fibers and phosphorylation of myosin light chain 10600496
Rat Vascular Smooth Muscle Cells Function Assay 10 μM 2 h Inhibits angiotensin II-induced hypertrophy 10642317
PC3 Function Assay 25 μM 1 h Induces morphological changes 10720471
PC3 Migration Assay 25 μM 1 h Inhibits the BMFB-CM and the EGF-stimulated migration 10720471
PC3 Growth Inhibition Assay 25 μM 17 h Does not inhibit cell growth 10720471
LNCaP Growth Inhibition Assay 25 μM 17 h Does not inhibit cell growth 10720471
Rat hepatic stellate cells Function Assay 30 μM 48 h Diminishes the phosphorylation of Erk2, and decreases new DNA synthesis 10845663
Pancreatic acinar cells Function Assay 10?μM 70 min Potentiates CCK-stimulated pancreatic enzyme secretion 12745080
C2C12 Function Assay 10?μM 6 h Prevents the serine phosphorylation of IRS-1 induced by insulin and/or TNF-α 16267124
PC 12 Function Assay 10?μM 24 h Attenuates catecholamine biosynthesis 16219424
Cynomolgus monkey embryonic stem cells Cytotoxic Assay 20 μM 24 h Promotes cyES cell survival 18940855
TSGH 8301 Migration Assay 20 μM 1 h Increases cell migration 19896475
Swiss3T3 Colony-forming Assay 10 μM 13 d Increases prostate cell colony-forming activity 21464902
HT22 Cytotoxic Assay 10 μM 13 h Protects against glutamate-induced neuronal death 22810835
Salivary gland stem cells Function Assay 10 μM 7 d Reduces SGSC senescence 25804560
Src-2 Growth Inhibition Assay 10 μM 18 d Does not inhibit cell growth 10021386
Src-1 Growth Inhibition Assay 10 μM 18 d Does not inhibit cell growth 10021386
NIH3T3 Growth Inhibition Assay 10 μM 18 d Does not inhibit cell growth 10021386
Src-4 Growth Inhibition Assay 10 μM 18 d Does not inhibit cell growth 10021386
Src-1 Growth Inhibition Assay 10 μM 18 d Does not inhibit cell growth 10021386
Ras-4 Growth Inhibition Assay 10 μM 18 d Strongly inhibits cell growth 10021386
Ras-2 Growth Inhibition Assay 10 μM 18 d Strongly inhibits cell growth 10021386
mNET1-e Growth Inhibition Assay 10 μM 18 d Strongly inhibits cell growth 10021386
mNET1-d Growth Inhibition Assay 10 μM 18 d Strongly inhibits cell growth 10021386
Dbl-e Growth Inhibition Assay 10 μM 18 d Moderately inhibits cell growth 10021386
Dbl-d Growth Inhibition Assay 10 μM 18 d Strongly inhibits cell growth 10021386
NIH3T3 Growth Inhibition Assay 10 μM 18 d Does not inhibit cell growth 10021386
Mesothelial cells from rat mesentery Invasive Assay 30 μM 20 h Blocks invasive activity 9930872
CCL39 Function Assay 30 μM 30 min Completely abolishes activation of Na-H exchanger NHE1 by integrins 9693382
HeLa Function Assay 10 μM 30 min Inhibits the formation of stress fibers and the assembly of vinculin-containing focal adhesions 9668072
N1E-115 Function Assay 10 μM 2 h Inhibits the assembly of microtubules and intermediate filaments to form extended processes 9647654
Swiss 3T3 cells Function Assay 10 μM 2 h Inhibits the assembly of microtubules and intermediate filaments to form extended processes 9647654
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生物活性

產(chǎn)品描述 Y-27632 2HCl是一種選擇性ROCK1和ROCK2抑制劑,無(wú)細(xì)胞試驗(yàn)中Ki分別為140 nM和300nM,比對(duì)其他激酶包括PKC,cAMP依賴性蛋白激酶,MLCK和PAK的作用強(qiáng)200多倍。
靶點(diǎn)
ROCK1 (p160ROCK) [1]
(Cell-free assay)
ROCK2 [6]
(Cell-free assay)
140 nM(Ki) 300 nM(Ki)
體外研究(In Vitro)
體外研究活性

Y-27632也同等有效抑制ROCK-II。Y-27632作用于PKC, cAMP依賴的蛋白激酶和 肌球蛋白輕鏈激酶(MLCK)幾乎沒(méi)有活性,Ki分別為26 μM, 25 μM, 和 > 250 μM。Y-27632通過(guò)選擇性抑制Ca2+敏感化,而抑制多種興奮劑而不是KCl,包括Phenylephrine, Histamine, Acetylcholine, Serotonin, Endothelin,和Thromboxane誘導(dǎo)的平滑肌收縮,IC50為0.3-1 μM。Y-27632 作用于培養(yǎng)的細(xì)胞,抑制Rho誘導(dǎo)的, p160ROCK調(diào)節(jié)的應(yīng)力纖維的形成。[1]

Y-27632處理,阻斷 Rho調(diào)節(jié)的肌動(dòng)球蛋白的激活,也阻斷LPA刺激的MM1 細(xì)胞入侵活性,這種作用存在濃度依賴性。[2]

10 μM Y-27632 處理在無(wú)血清懸浮(SFEB)培養(yǎng)基中的人類胚胎干細(xì)胞(hES),顯著減少分離誘導(dǎo)的凋亡,提高克隆效率(從~1%提高到~27%), 轉(zhuǎn)基因后促進(jìn)亞克隆,且使SFEB培養(yǎng)的hES細(xì)胞存活及分化成Bf1+皮質(zhì)和基底端腦祖細(xì)胞。[5]

實(shí)驗(yàn)圖片 檢測(cè)方法 檢測(cè)指標(biāo) 實(shí)驗(yàn)圖片 PMID
Western Blot p-LIMK1(Thr508) p-LIMK2(Thr505) p-Cofilin(Ser3) CDK2 KRT7 ROCK2 E-cadherin p-MLC2(Ser19) 24704720
Transwell migration assay cell migration inhibition 27694793
Immunofluorescence Neurotoxicity Assay E-cadherin beta-catenin Phalloidin 21362567
Growth inhibition assay cell proliferation 24523903
ELISA caspase-9 30320378
體內(nèi)研究(In Vivo)
體內(nèi)研究活性

Y-27632按30 mg/kg劑量口服處理自發(fā)性高血壓大鼠,腎性高血壓大鼠,及去氧皮質(zhì)酮醋酸(DOCA)鹽高血壓大鼠,顯著降低血壓,這種作用存在劑量依賴性。[1]

Y-27632按每小時(shí)0.55 μL通過(guò)植入泵持續(xù)處理表達(dá)Val14-RhoA的大鼠,持續(xù)11天,延遲 MM1 細(xì)胞入侵。[2]

Y-27632作用于肺循環(huán),通過(guò)抑制ROCK, 降低 缺氧誘導(dǎo)的血管生成,和血管重構(gòu)。[4]

動(dòng)物實(shí)驗(yàn) Animal Models 攜帶自發(fā)或誘發(fā)高血壓的雄性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 口服處理 (大鼠);ip(小鼠)

化學(xué)信息&溶解度

分子量 320.26 分子式

C14H21N3O.2HCl

CAS號(hào) 129830-38-2 SDF Download Y-27632 2HCl SDF
Smiles CC(C1CCC(CC1)C(=O)NC2=CC=NC=C2)N.Cl.Cl
儲(chǔ)存條件(自收到貨起)

體外溶解度
批次:

DMSO : 64 mg/mL ( (199.83 mM) ;DMSO吸濕會(huì)降低化合物溶解度,請(qǐng)使用新開(kāi)封DMSO)

Water : 64 mg/mL (199.83 mM)

Ethanol : 4 mg/mL (12.48 mM)

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次:

現(xiàn)配現(xiàn)用,請(qǐng)按從左到右的順序依次添加,澄清后再加入下一溶劑

動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器(澄清溶液)

第一步:請(qǐng)輸入基本實(shí)驗(yàn)信息(考慮到實(shí)驗(yàn)過(guò)程中的損耗,建議多配一只動(dòng)物的藥量)

mg/kg g μL

第二步:請(qǐng)輸入動(dòng)物體內(nèi)配方組成(配方適用于不溶于水的藥物;不同批次藥物配方比例不同,請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)算結(jié)果:

工作液濃度: mg/ml;

DMSO母液配制方法: mg 藥物溶于μL DMSO溶液(母液濃度mg/mL,:如該濃度超過(guò)該批次藥物DMSO溶解度,請(qǐng)先聯(lián)系Selleck);

體內(nèi)配方配制方法:μL DMSO母液,加入μL PEG300,混勻澄清后加入μL Tween 80,混勻澄清后加入μL ddH2O,混勻澄清。

體內(nèi)配方配制方法:μL DMSO母液,加入μL Corn oil,混勻澄清。

注意:1. 首先保證母液是澄清的;
2.一定要按照順序依次將溶劑加入,進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液,可采用渦旋、超聲或水浴加熱等物理方法助溶。

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常見(jiàn)問(wèn)題及建議解決方法

問(wèn)題 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.

問(wèn)題 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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