Home Cell Cycle ROCK inhibitor Thiazovivin For research use only.

Thiazovivin

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

Thiazovivin Chemical Structure

Thiazovivin Chemical Structure

CAS No. 1226056-71-8

Purity & Quality Control

Products often used together with Thiazovivin

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 Related Products

Signaling Pathway

ROCK Signaling Pathways

ROCK Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HSMCs Function Assay 1 μM 2 h reverses AngII-induced MYPT1 phosphorylation 24965170
SCU-i10 hiPSCs Growth Inhibition Assay 0-20 μM 24 h significantly modulates single-cell plating efficiency and promote NCM growth 25077932
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
Click to View More Cell Line Experimental Data

Biological Activity

Description 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
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).
Cell Research Cell lines ASZ001 cells
Concentrations 0.5 μM
Incubation Time 72 h
Method

Cells were treated with various concnetrations of thiazovivin.
Experimental Result Images Methods Biomarkers Images PMID
Western blot ROCK1/2 28849097
Immunofluorescence E-cadherin / N-cadherin / α-SMA 28849097

Chemical Information & Solubility

Molecular Weight 311.36 Formula

C15H13N5OS
CAS No. 1226056-71-8 SDF Download Thiazovivin SDF
Smiles C1=CC=C(C=C1)CNC(=O)C2=CSC(=N2)NC3=NC=NC=C3
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 63 mg/mL ( (202.33 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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