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Thiazovivin is a selective small molecule Rho-associated kinase (ROCK) inhibitor. When used in combination with ALK5 inhibitor SB-431542 and MEK inhibitor PD-0325901 , it significantly improves (200-fold) the efficiency of iPSC generation from human fibroblast reprogramming. Thiazovivin also improves the survival of human embryonic stem cells upon trypsinization. More over, by regulating E-cadherin mediated cell-cell interaction, Thiazovivin can protects human ES cells from death in the absence of ECM.
| Cell Experiment | |
|---|---|
| Cell lines | hESCs cells |
| Preparation method | For clonal survival assays, single hESCs were diluted to clonal density and plated onto 96-well Matrigel-coated plate. For lowdensity survival assays, 500 cells were plated onto 96-well Matrigelcoated plate. To visualize hESC colonies, cultures were fixed in 4% paraformaldehyde in phosphate buffered saline (PBS) for 5 min, washed once in PBS, then stained for alkaline phosphatase (ALP) activity as described in the manufacturer’s instructions. ALP positive colonies were counted on an inverted microscope. |
| Concentrations | 2 μM |
| Incubation time | 4 days |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 311.36 |
| Formula | C15H13N5OS |
| CAS Number | 1226056-71-8 |
| Solubility (25°C) | DMSO 25 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Best-selling ROCK Products |
|---|
| Y-27632 dihydrochloride
Y-27632 is a potent, selective inhibitor of Rho-associated protein kinases (ROCK) with IC50 values of 140-220 nM for ROCK1 and ROCK2. In addition, Y-27632 inhibited LPA-induced entosis. |
| H-1152
H-1152, an isoquinolinesulfonamide derivative, is a more specific, stronger and membrane-permeable inhibitor of Rho-kinase with a Ki value of 1.6 nM, but poor inhibitor of other serine/threonine kinases. |
| Y-39983 dihydrochloride
Y-39983 (Y-33075) dihydrochloride is a selective ROCK inhibitor with an IC50 of 3.6 nM, derived from Y-27632, inhibited ROCK more potently than Y-27632. |
| GSK269962A
GSK269962A is a potent ROCK inhibitor with IC50 values of 1.6 and 4 nM for recombinant human ROCK1 and ROCK2, respectively. |
| TC-S 7001
BAY-549 (TC-S 7001) is a potent and highly selective, orally active ROCK inhibitor, with IC50 values of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2, respectively. |
| Other ROCK Products |
|---|
| Fasudil hydrochloride
Fasudil hydrochloride is a potent Rho-associated kinase inhibitor with IC50 of 10.7 μM. |
| RKI-1447
RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 6 nM, respectively. |
| GSK429286A
GSK429286A is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively. |
| Fasudil
Fasudil (HA-1077) is a potent inhibitor of ROCK-II, PKA, PKG, PKC, and MLCK with Ki of 0.33 μM, 1.6 μM, 1.6 μM, 3.3 μM and 36 μM, respectively. |
| RKI-1313
Inhibition of ROCK in human H1299 cells assessed as decrease in phosphorylation of MYPT-1 after 1 hr by Western immunoblotting assay. |
| Hydroxyfasudil hydrochloride
Hydroxyfasudil (HA-1100), an active metabolite of fasudil hydrochloride, is a specific Rho-kinase(ROCK) inhibitor with IC50 values of 0.73 μM and 0.72 μM for ROCK1 and ROCK2, respectively. |
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Products are for research use only. Not for human use. We do not sell to patients.
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