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 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.|
|Incubation time||4 days|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO ≥60 mg/mL|
Direct conversion of porcine embryonic fibroblasts into adipocytes by chemical molecules.
Zhu et al. Cell Reprogram. 2012 Apr;14(2):99-105. PMID: 22372576.
|Related ROCK Products|
ZINC00881524 is a potent and selective ROCK inhibitor.
|Ripasudil (K-115) dihydrate
Ripasudil (K-115) hydrochloride dihydrate is potent ROCK inhibitor with IC50 of 51 nM and 19 nM for ROCK1 and ROCK2, respectively, used for the treatment of glaucoma and ocular hypertension.
SR-3677 is a new potent and selective ROCK-II inhibitor with an IC50 of ~3 nM in enzyme and cell based assays; IC50 for ROCK-I is 56 ± 12 nM.
GSK180736A, developed as a Rho-associated, coiled-coil-containing protein kinase inhibitor, binds to GRK2(G protein-coupled receptor kinase 2) with logIC50 pf -6.6 (logIC50 -4.0 for GRK5 and >-3 for GRK1); ≥400-fold selective for GRK2 over both GRK1 and GRK5.
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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