Thiazovivin

製品コード：S1459 純度：99.85%

Thiazovivin is a novel ROCK inhibitor with IC50 of 0.5 μM in a cell-free assay, promotes hESC survival after single-cell dissociation.

CAS No. 1226056-71-8

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
5mg	JPY 22000	国内在庫あり
10mg	JPY 37000	国内在庫あり
50mg	JPY 100500	国内在庫あり
1g	JPY 448500	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（80）

製品安全説明書

現在のバッチを見る：純度： 99.85%

99.85

Thiazovivinと併用されることが多い化合物

SB431542

Thiazovivin and SB431542 combination use allows porcine embryonic fibroblasts (PEFs) to directly convert to fat-laden adipocytes.

Zhu J, et al. Cell Reprogram. 2012 Apr;14(2):99-105.

Y-27632

Thiazovivin and Y-27632 combined use maintains the undifferentiated state of iPSCs and promotes cell survival.

Mohseni R, et al. Cell Biol Int. 2015 May;39(5):515-8.

RepSox (E-616452)

Thiazovivin and RepSox lead to significant decrease in COL1A1 expression levels in HSF and KSF cells.

Yeo DC, et al. ACS Appl Bio Mater. 2018 Dec 17;1(6):2054-2061.

Laduviglusib (CHIR-99021)

Thiazovivin and Laduviglusib incubation in Lgr5-GFPhi cells results in colony formation by 25% to 30% of single-sorted intestinal stem cells (ISCs).

Wang F, et al. Gastroenterology. 2013 Aug;145(2):383-95.e1-21.

Thiazovivin関連製品

関連ターゲット	ROCK1 ROCK2	もっと見る
関連製品	Y-27632 2HCl Y-27632 Fasudil HCl GSK429286A RKI-1447 GSK269962A HCl Y-39983 Dihydrochloride Hydroxyfasudil HCl	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
SCU-i10 hiPSCs	Growth Inhibition Assay	0-20 μM	24 h	significantly modulates single-cell plating efficiency and promote NCM growth	25077932
HSMCs	Function Assay	1 μM	2 h	reverses AngII-induced MYPT1 phosphorylation	24965170
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
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生物活性

製品説明

Thiazovivin is a novel ROCK inhibitor with IC50 of 0.5 μM in a cell-free assay, promotes hESC survival after single-cell dissociation.

Targets

ROCK ^[1]
(Cell-free assay)

~0.5 μM

In Vitro
In vitro	Although displaying little impact on cell proliferation, Thiazovivin treatment significantly enhances the survival of human embryonic stem cells (hESCs) after enzymatic dissociation more than 30-fold, while homogenously maintaining pluripotency with the characteristic colony morphology, expression of typical pluripotency markers such as alkaline phosphatase (ALP), and normal karyotype. Dissociated hESCs treated with Thiazovivin display dramatically increased adhesion to matrigel- or laminin-coated plates but not to gelatin-coated plates within a few hours. Thiazovivin treatment increases cell-ECM adhesion-mediated β1 integrin activity, which synergizes with growth factors to promote cell survival. In addition to activating integrin, Thiazovivin but not Tyrintegin (Ptn) protects hESCs from death in the absence of ECM in suspension through E-cadherin-mediated cell-cell interaction. Thiazovivin treatment potently inhibits endocytosis of E-cadherin, consequently stabilizing E-cadherin on the cell surface and leading to reestablishment of cell-cell interaction, which is essential for hESC survival in ECM-free conditions. Thiazovivin but not Tyrintegin (Ptn) at 2 μM inhibits Rho-associated kinase (ROCK) activity and protects hESCs at a similar level as the widely used selective ROCK inhibitor Y-27632 at 10 μM, suggesting that Rho-ROCK signaling regulates cell-ECM and cell-cell adhesion. ^[1] Thiazovivin at 1 μM increases the reprogramming efficiency of CB mononuclear cells to induced pluripotent stem cells (iPSCs) by more than 10 times. ^[2]
Kinase Assay	In vitro ROCK assay
Kinase Assay	Thiazovivin is dissolved in DMSO. CycLex Rho-kinase assay kit is used to detect ROCK activity using recombinant ROCK in the presence of increasing concentrations of Thiazovivin (~10 μM).
細胞実験	細胞株	ASZ001 cells
	濃度	0.5 μM
	反応時間	72 h
	実験の流れ	Cells were treated with various concnetrations of thiazovivin.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	ROCK1/2		28849097
	Immunofluorescence	E-cadherin / N-cadherin / α-SMA		28849097

参考
[1] Xu Y, et al. Proc Natl Acad Sci U S A, 2010, 107(18), 8129-8134. [2] Hu K, et al. Blood, 2011, 117(14), e109-119. [3] Lin T, et al. Nat Methods, 2009, 6(11), 805-808. [4] Whitson RJ, et al. Nat Med. 2018 Mar;24(3):271-281. + 展開

参考

[4] Whitson RJ, et al. Nat Med. 2018 Mar;24(3):271-281.

+ 展開

化学情報

分子量	311.36	化学式	C₁₅H₁₃N₅OS
CAS No.	1226056-71-8	SDF	Download Thiazovivin SDFをダウンロードする
Smiles	C1=CC=C(C=C1)CNC(=O)C2=CSC(=N2)NC3=NC=NC=C3
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 : 63 mg/mL ( (202.33 mM)；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 : Insoluble

Ethanol : Insoluble

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。

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