Thiazovivin

Catalog No.S1459

Thiazovivin Chemical Structure

Molecular Weight(MW): 311.36

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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In DMSO USD 150 In stock
USD 120 In stock
USD 210 In stock
USD 670 In stock
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Cited by 31 Publications

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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

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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SCU-i10 hiPSCs MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWmwMVIxKM7:TR?= MonONlQhcA>? MnrEd4lodmmoaXPhcpRtgSCvb3T1cIF1\XNic3nu[4xmNWOnbHygdIxifGmwZzDl[oZq[2mnbnP5JIFv\CCycn;tc5RmKE6FTTDndo94fGh? MlTENlUxPzd7M{K=
HSMCs NU\BcJNsTnWwY4Tpc44hSXO|YYm= NITWPXYy6oDLzszN M4DXT|IhcA>? NXjBeo5semW4ZYLz[ZMhSW6pSVmtbY5lfWOnZDDNXXBVOSCyaH;zdIhwenmuYYTpc44> MonhNlQ6PjVzN{C=

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
ROCK1/2; 

PubMed: 28849097     


Protein expression of ROCK1/2 in HCECs cultured with 4 µM TZV for different periods of time, n=3. HCECs, human corneal endothelial cells; TZV, thiazovivin.

28849097
Immunofluorescence
E-cadherin / N-cadherin / α-SMA; 

PubMed: 28849097     


Function-related protein expression in primary HCECs cultured with various concentrations of TZV for 24 h, n=3. (A) E-cadherin, N-cadherin, and α-SMA immunostaining (magnification, ×200);

28849097

Protocol

Solubility (25°C)

In vitro DMSO 15 mg/mL (48.17 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing. 		30 mg/mL

* 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 Information

Molecular Weight 311.36
Formula

C15H13N5OS
CAS No. 1226056-71-8
Storage powder
in solvent
Synonyms N/A

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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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ROCK Signaling Pathway Map

ROCK Inhibitors with Unique Features

  • Selective ROCK Inhibitor

    Fasudil (HA-1077) HCl : ROCK-II-selective, Ki=0.33 μM.

  • Most Potent ROCK Inhibitor

    GSK429286A : ROCK1, IC50=14 nM; ROCK2, IC50=63 nM.

  • ROCK Inhibitor in Clinical Trial

    Fasudil (HA-1077) HCl : Phase III for scleroderma.

  • Newest ROCK Inhibitor

    RKI-1447 : Highly potent inhibitor of?b>ROCK1燼nd?b>ROCK2, with?b>IC50爋f 14.5 nM and 6.2 nM, respectively.

Related ROCK Products

  • Ro-3306 New

    RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with Ki of 20 nM, >15-fold selectivity against a diverse panel of human kinases.

  • CCG-1423 New

    CCG-1423 is a specific RhoA pathway inhibitor, which inhibits SRF-mediated transcription.

  • ML141 New

    ML141 (CID-2950007), is demonstrated to be a potent, selective and reversible non-competitive inhibitor of Cdc42 GTPase suitable for in vitro assays, with IC50 of 200 nM and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7).

  • Y-27632 2HCl

    Y-27632 2HCl is a selective ROCK1 (p160ROCK) inhibitor with Ki of 140 nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.

  • GSK429286A

    GSK429286A is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively.

    Features:Greater selectivity than Y-27632.

  • Fasudil (HA-1077) HCl

    Fasudil(HA-1077), a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively.

  • RKI-1447

    RKI-1447 is a potent inhibitor of ROCK1 and ROCK2, with IC50 of 14.5 nM and 6.2 nM, respectively, has anti-invasive and antitumor activities.

  • Palbociclib (PD-0332991) HCl

    Palbociclib (PD-0332991) HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.

    Features:Non-cytotoxic, and halts cancer cell growth & could be used in glioblastoma that has relapsed after temozolomide treatment (a chemotherapeutic used to treat many cancers).

  • Alisertib (MLN8237)

    Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Phase 3.

    Features:First orally available inhibitor of Aurora A.

  • Adavosertib （MK-1775）

    MK-1775 is a potent and selective Wee1 inhibitor with IC50 of 5.2 nM in a cell-free assay; hinders G2 DNA damage checkpoint. Phase 2.

    Features:The first reported Wee1 inhibitor.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID