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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
| Related ROCK Products |
|---|
| Akt/ROCK-IN-1
Akt/ROCK-IN-1 (B12) is a dual inhibitor for Akt and ROCK, with the IC50s of 0.023 nM and 1.47 nM, respectively. |
| Scaff10-8
Scaff10-8, bound to RhoA, inhibits the AKAP-Lbc-mediated RhoA activation. |
| ROCK-IN-6
ROCK-IN-6 is a potent and selectiveROCK2 inhibitor with an IC50 of 2.19 nM. |
| ROCK-IN-4
ROCK-IN-4 is a potent ROCK inhibitor maintaining NO releasing ability. |
| ROCK-IN-32
ROCK-IN-32 is a ROCK inhibitor, with an IC50 value of 11 nM for ROCK2. |
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