Y-27632 2HCl

製品コード：S1049 純度：99.89%

Y-27632 2HCl は選択的 ROCK1 (p160ROCK) 阻害剤であり、cell-free assay における K_i は 140 nM です。PKC, cAMP-依存性プロテインキナーゼ, MLCK や PAK など他のキナーゼよりも ROCK1 に対して 200 倍以上の選択性を示します。

CAS No. 129830-38-2

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 41500	国内在庫あり
2mg	JPY 22000	国内在庫あり
5mg	JPY 29500	国内在庫あり
10mg	JPY 41500	国内在庫あり
50mg	JPY 85500	国内在庫あり
200mg	JPY 145500	国内在庫あり
1g	JPY 295500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（1123）

製品安全説明書

現在のバッチを見る：純度： 99.89%

99.89

Y-27632 2HClと併用されることが多い化合物

SB202190

Y-27632 2HCl and SB202190, along with other small molecule inhibitors, generate inducible mesenchymal stromal/stem cells (MSCs)-like cells (iMSCs) from human primary dermal fibroblasts.

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

SB431542

Y-27632 2HCl and SB431542 combination reverses the mesenchymal actin cytoskeleton stress fibers induced by TGF-β1 in TGF-β1 knockout mice cells (mTEC-KO).

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

Laduviglusib (CHIR-99021)

Y-27632 2HCl and CHIR99021 collectively reduce the expression of adipogenic genes in both wild-type (WT) and PKP2^mut cardiac myocytes (CMs).

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

MG132

Y-27632 reduces P-IκBα polyubiquitination caused by TNFα with MG132 pre-treatment in MYLA cells.

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

Z-VAD-FMK

Y27632 2HCl and Z-VAD-FMK block membrane blebbing and nucleus condensation induced by H2O2 in PC12 cells.

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

Y-27632 2HCl関連製品

関連ターゲット	ROCK1 ROCK2	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library PI3K/Akt Inhibitor Library MAPK Inhibitor Library DNA Damage/DNA Repair compound Library Cell Cycle compound library	もっと見る

シグナル伝達経路

ROCKシグナル伝達経路

ROCK阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
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
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明

Targets

ROCK1 (p160ROCK) ^[1] (Cell-free assay)	ROCK2 ^[6] (Cell-free assay)
140 nM(Ki)	300 nM(Ki)

In Vitro
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 K_i 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]
Kinase Assay	Phosphorylation reactions
Kinase Assay	The p160ROCK is expressed in COS cells as tagged full-length proteins, and immunoprecipitated by the use of anti-tag antibodies. The p160ROCK (30 ng) is incubated with 40 μM [γ-³²P]ATP (3.3 Ci/mmol) and with 3 μg of either histone (HF2A), dephosphorylated casein or MBP in the presence of various concentrations of Y-27632 2HCl at 30 °C in a total volume of 31 μL. A 7 μL aliquot is taken at 0, 5, 10, and 20 minutes, mixed with an equal volume of 2 × Laemmli sample buffer, and applied to SDS-PAGE. The gel is stained with Commassie Blue, dried and subjected to analysis by a Bioimage Analyzer BAS2000. The Y-27632 2HCl concentration required to inhibit p160ROCK activity by 50% (IC50 value) is obtained. K_i value is calculated according to the equation, K_i = IC50/(1 + S/K_m), where S and K_m represent concentrations of and K_m value for ATP.
細胞実験	細胞株	hES Cells
	濃度	10 uM
	反応時間	1 h
	実験の流れ	Y-27632 was added to culture medium at 10 uM 1 h before detaching the cells from the feeder layer and also upon seeding the cells onto a new MEF layer.
実験結果図	Methods	Biomarkers	結果図	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

In Vivo
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]
動物実験	動物モデル	Male Wistar rats with spontaneous or induced hypertension; Swiss albino mice with Ehrlich ascites carcinoma
	投与量	30 mg/kg/day (Rat); 0-10 mg/kg (mice)
	投与経路	Orally (Rat); i.p. (Mice)

参考
[1] Uehata M, et al. Nature, 1997, 389(6654), 990-994. [2] Itoh K, et al. Nat Med, 1999, 5(2), 221-225. [3] Bito H, et al. Neuron, 2000, 26(2), 431-441. [4] Watanabe K, et al. Nat Biotechnol, 2007, 25(6), 681-686. [5] Hyvelin JM, et al. Circ Res, 2005, 97(2), 185-191. [6] Ishizaki T, et al. Mol Pharmacol. 2000, 57(5), 976-983. [7] Isler D, et al. Pharmacol Rep. 2014, 66(1), 114-120. + 展開

参考

+ 展開

化学情報

分子量	320.26	化学式	C₁₄H₂₁N₃O.2HCl
CAS No.	129830-38-2	SDF	Download Y-27632 2HCl SDFをダウンロードする
Smiles	CC(C1CCC(CC1)C(=O)NC2=CC=NC=C2)N.Cl.Cl
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 64 mg/mL ( (199.83 mM)； Warmed with 50℃ water bath; 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : 64 mg/mL

Ethanol : 4 mg/mL

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

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Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

よくある質問（FAQ）

質問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.

質問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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