Thiazovivin

Catalog No.S1459

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

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Thiazovivin Chemical Structure

Thiazovivin Chemical Structure
Molecular Weight: 311.36

Validation & Quality Control

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Quality Control & MSDS

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Product Information

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  • Research Area
  • Combination Therapy
    Combination Therapy

Product Description

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)
IC50 ~0.5 μM
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]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
SCU-i10 hiPSCsNIDnNJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MmrnNE0zOCEQvF2=MYmyOEBpM{TPVpNq\26rZnnjZY51dHlibX;keYxifGW|IIPpcodt\S2lZXzsJJBt[XSrbneg[YZncWOrZX7jfUBidmRicILvcY91\SCQQ12g[5Jwf3SqM1;pR|I2ODd5OUOy
HSMCsMXfGeY5kfGmxbjDBd5NigQ>?Mk\hNgKBkc7:TR?=MViyJIg>MYry[ZZmenOnczDBcodKUS2rbnT1Z4VlKE2\UGSxJJBpd3OyaH;yfYxifGmxbh?=NIfGdYQzPDl4NUG3NC=>

... Click to View More Cell Line Experimental Data

In vivo
Features

Protocol(Only for Reference)

Kinase Assay:

[1]

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).

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[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.

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Chemical Information

Download Thiazovivin SDF
Molecular Weight (MW) 311.36
Formula

C15H13N5OS

CAS No. 1226056-71-8
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 15 mg/mL (48.17 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name N-benzyl-2-(pyrimidin-4-ylamino)thiazole-4-carboxamide

Customer Product Validation(1)


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Rating
Source Arch Toxicol 2013 87(12), 2215-31. Thiazovivin purchased from Selleck
Method Cellomics Array Scan
Cell Lines LUHMES human neuronal precursor cells
Concentrations
Incubation Time 24 h
Results Thiazovivin accelerated neurite growth significantly.

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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